Detailed description page of THPdb

Details of Th1006 which contains 6 entries.

Entry 1
(1) Primary information
ID 1032
ThPP ID Th1006
Therapeutic Peptide/Protein Name Bivalirudin
Sequence FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification Ia
Molecular Weight 2180.2853
Chemical Formula C98H138N24O33
Isoelectric Point 3.91
Hydrophobicity -0.985
Melting Point (℃) N.A.
Half Life Normal renal function: 0.42 hours (in normal conditions)
Description Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism 80% proteolytic cleavage
Absorption Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution 0.2L/kg
Clearance 3.4 mL/min/kg [Normal renal function]
Categories Antithrombins
Patents Number US7582727
Date of Issue 27/01/09
Date of Expiry 27/01/29
Drug Interaction Deferasirox, Anticoagulants increase the risk for gastrointestinal ulceration/irritation and/or GI bleeding. If these two agents must be used, patients need to be closely monitored for signs and symptoms of GI toxicity.
Target Prothrombin
Information of corresponding available drug in the market
Brand Name Angiomax
Company Medicines Co or MDCO
Brand Discription Angiomax is a specific and reversible thrombin inhibitor. The active substance is a synthetic, 20 amino acid peptide with a molecular weight of 2180 daltons (anhydrous free base peptide).
Prescribed for It is used for thinning the blood in patients with unstable angina who are undergoing percutaneous transluminal coronary angioplasty (PTCA) and in patients undergoing percutaneous coronary intervention (PCI).
Chemical Name D-phenylalanyl-L-prolyl-L-arginyl-L-prolyl-glycylglycyl-glycyl-glycyl-L-asparagyl-glycyl-L-aspartyl-L-phenylalanyl-L-glutamyl-L-glutamyl-L-isoleucyl-L-prolyl-L-glutamyl-L-glutamyl-L-tyrosyl-L-leucine trifluoroacetate (salt) hydrate
Formulation Each vial contains 250 mg bivalirudin, 125 mg mannitol, and sodium hydroxide to adjust the pH to 5-6 (equivalent of approximately 12.5 mg sodium). When reconstituted with Sterile Water for Injection, the product yields a clear to opalescent, colorless to
Physcial Appearance Supplied in single-use vials as a white lyophilized cake
Route of Administration Intravenous infusion
Recommended Dosage Intravenous (IV) bolus dose of 0.75Â mg/kg, followed by an infusion of 1.75Â mg/kg/h for the duration of the PCI/PTCA procedure.
Contraindication Allergic and have major active bleeding
Side Effects Anxiety; back, stomach, or pelvic pain; headache; nausea; nervousness; pain at the injection site; trouble sleeping; upset stomach; vomiting. And severe side effect may include Severe allergic reactions (rash; hives; itching; difficulty breathing.
Useful Link http://reference.medscape.com/drug/angiomax-angiox-bivalirudin-342137
PubMed ID 17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure Th1006 (View) or (Download)

Entry 2
(2) Primary information
ID 1033
ThPP ID Th1006
Therapeutic Peptide/Protein Name Bivalirudin
Sequence FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification Ia
Molecular Weight 2180.2853
Chemical Formula C98H138N24O33
Isoelectric Point 3.91
Hydrophobicity -0.985
Melting Point (℃) N.A.
Half Life Creatinine clearance 10-29mL/min: 0.95 hours
Description Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism 80% proteolytic cleavage
Absorption Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution 0.2L/kg
Clearance 3.4 mL/min/kg [mild renal function]
Categories Antithrombins
Patents Number US5196404
Date of Issue 23/05/93
Date of Expiry 23/05/10
Drug Interaction Gemcitabine, Gemcitabine may enhance the adverse/toxic effect of Bleomycin. The risk of pulmonary toxicity may be increased. Use extreme caution if using gemcitabine and bleomycin in combination. Monitor for the development of pulmonary toxicity
Target N.A.
Information of corresponding available drug in the market
Brand Name Angiox
Company The Medicines Company UK Ltd
Brand Discription N.A.
Prescribed for Used as an anticoagulant in adult patients undergoing percutaneous coronary intervention (PCI), including patients with ST-segment elevation myocardial infarction (STEMI) undergoing primary PCI. Angiox is also indicated for the treatment of adult patients
Chemical Name N.A.
Formulation Each vial contains 250 mg bivalirudin.
Physcial Appearance Powder for concentrated solution
Route of Administration Injection
Recommended Dosage 0.75 mg/kg IV bolus, initially, followed by continuous infusion at rate of 1.75 mg/kg/hr for duration of procedure
Contraindication Hypersensitivity, active bleeding or increased risk of bleeding because of haemostasis disorder or irreversible coagulation disorder, uncontrolled hypertension, subacute bacterial endocarditis, severe renal impairment and in dialysis dependent pateints,
Side Effects N.A.
Useful Link http://www.rxlist.com/angiomax-drug.htm
PubMed ID 17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure Th1006 (View) or (Download)

Entry 3
(3) Primary information
ID 1034
ThPP ID Th1006
Therapeutic Peptide/Protein Name Bivalirudin
Sequence FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification Ia
Molecular Weight 2180.2853
Chemical Formula C98H138N24O33
Isoelectric Point 3.91
Hydrophobicity -0.985
Melting Point (℃) N.A.
Half Life Dialysis-dependant patients: 3.5 hours
Description Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism 80% proteolytic cleavage
Absorption Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution 0.2L/kg
Clearance 2.7 mL/min/kg [moderate renal function]
Categories Antithrombins
Patents Number CA2065150
Date of Issue 14/12/99
Date of Expiry 17/08/10
Drug Interaction Ginkgo biloba, Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
Target N.A.
Information of corresponding available drug in the market
Brand Name N.A.
Company N.A.
Brand Discription N.A.
Prescribed for N.A.
Chemical Name N.A.
Formulation N.A.
Physcial Appearance N.A.
Route of Administration N.A.
Recommended Dosage N.A.
Contraindication N.A.
Side Effects N.A.
Useful Link https://www.medicines.org.uk/emc/medicine/16741
PubMed ID 17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure Th1006 (View) or (Download)

Entry 4
(4) Primary information
ID 1035
ThPP ID Th1006
Therapeutic Peptide/Protein Name Bivalirudin
Sequence FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification Ia
Molecular Weight 2180.2853
Chemical Formula C98H138N24O33
Isoelectric Point 3.91
Hydrophobicity -0.985
Melting Point (℃) N.A.
Half Life N.A.
Description Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism 80% proteolytic cleavage
Absorption Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution 0.2L/kg
Clearance 2.8 mL/min/kg [severe renal function]
Categories Antithrombins
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction Rivaroxaban, Anticoagulants may enhance the anticoagulant effect of rivaroxaban. Avoid concurrent use of rivaroxaban with other anticoagulants whenever possible, other than during transition periods, due to the possible increased for bleeding.
Target N.A.
Information of corresponding available drug in the market
Brand Name N.A.
Company N.A.
Brand Discription N.A.
Prescribed for N.A.
Chemical Name N.A.
Formulation N.A.
Physcial Appearance N.A.
Route of Administration N.A.
Recommended Dosage N.A.
Contraindication N.A.
Side Effects N.A.
Useful Link http://www.drugs.com/cdi/angiomax.html
PubMed ID 17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure Th1006 (View) or (Download)

Entry 5
(5) Primary information
ID 1036
ThPP ID Th1006
Therapeutic Peptide/Protein Name Bivalirudin
Sequence FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification Ia
Molecular Weight 2180.2853
Chemical Formula C98H138N24O33
Isoelectric Point 3.91
Hydrophobicity -0.985
Melting Point (℃) N.A.
Half Life N.A.
Description Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism 80% proteolytic cleavage
Absorption Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution 0.2L/kg
Clearance 1 mL/min/kg [Dialysis-dependent patients]
Categories Antithrombins
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction Treprostinil, The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Bivalirudin. Monitor for increased bleeding during concomitant thearpy.
Target N.A.
Information of corresponding available drug in the market
Brand Name N.A.
Company N.A.
Brand Discription N.A.
Prescribed for N.A.
Chemical Name N.A.
Formulation N.A.
Physcial Appearance N.A.
Route of Administration N.A.
Recommended Dosage N.A.
Contraindication N.A.
Side Effects N.A.
Useful Link http://www.angiomax.com/
PubMed ID 17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure Th1006 (View) or (Download)

Entry 6
(6) Primary information
ID 1037
ThPP ID Th1006
Therapeutic Peptide/Protein Name Bivalirudin
Sequence FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification Ia
Molecular Weight 2180.2853
Chemical Formula C98H138N24O33
Isoelectric Point 3.91
Hydrophobicity -0.985
Melting Point (℃) N.A.
Half Life N.A.
Description Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism 80% proteolytic cleavage
Absorption Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution 0.2L/kg
Clearance N.A.
Categories Antithrombins
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction N.A.
Target N.A.
Information of corresponding available drug in the market
Brand Name N.A.
Company N.A.
Brand Discription N.A.
Prescribed for N.A.
Chemical Name N.A.
Formulation N.A.
Physcial Appearance N.A.
Route of Administration N.A.
Recommended Dosage N.A.
Contraindication N.A.
Side Effects N.A.
Useful Link N.A.
PubMed ID 17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure Th1006 (View) or (Download)

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

(1) Primary information
Entry 1
ID	1032
ThPP ID	Th1006
Therapeutic Peptide/Protein Name	Bivalirudin
Sequence	FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification	Ia
Molecular Weight	2180.2853
Chemical Formula	C98H138N24O33
Isoelectric Point	3.91
Hydrophobicity	-0.985
Melting Point (℃)	N.A.
Half Life	Normal renal function: 0.42 hours (in normal conditions)
Description	Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease	For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics	Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action	Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity	Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism	80% proteolytic cleavage
Absorption	Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution	0.2L/kg
Clearance	3.4 mL/min/kg [Normal renal function]
Categories	Antithrombins
Patents Number	US7582727
Date of Issue	27/01/09
Date of Expiry	27/01/29
Drug Interaction	Deferasirox, Anticoagulants increase the risk for gastrointestinal ulceration/irritation and/or GI bleeding. If these two agents must be used, patients need to be closely monitored for signs and symptoms of GI toxicity.
Target	Prothrombin
Information of corresponding available drug in the market
Brand Name	Angiomax
Company	Medicines Co or MDCO
Brand Discription	Angiomax is a specific and reversible thrombin inhibitor. The active substance is a synthetic, 20 amino acid peptide with a molecular weight of 2180 daltons (anhydrous free base peptide).
Prescribed for	It is used for thinning the blood in patients with unstable angina who are undergoing percutaneous transluminal coronary angioplasty (PTCA) and in patients undergoing percutaneous coronary intervention (PCI).
Chemical Name	D-phenylalanyl-L-prolyl-L-arginyl-L-prolyl-glycylglycyl-glycyl-glycyl-L-asparagyl-glycyl-L-aspartyl-L-phenylalanyl-L-glutamyl-L-glutamyl-L-isoleucyl-L-prolyl-L-glutamyl-L-glutamyl-L-tyrosyl-L-leucine trifluoroacetate (salt) hydrate
Formulation	Each vial contains 250 mg bivalirudin, 125 mg mannitol, and sodium hydroxide to adjust the pH to 5-6 (equivalent of approximately 12.5 mg sodium). When reconstituted with Sterile Water for Injection, the product yields a clear to opalescent, colorless to
Physcial Appearance	Supplied in single-use vials as a white lyophilized cake
Route of Administration	Intravenous infusion
Recommended Dosage	Intravenous (IV) bolus dose of 0.75Â mg/kg, followed by an infusion of 1.75Â mg/kg/h for the duration of the PCI/PTCA procedure.
Contraindication	Allergic and have major active bleeding
Side Effects	Anxiety; back, stomach, or pelvic pain; headache; nausea; nervousness; pain at the injection site; trouble sleeping; upset stomach; vomiting. And severe side effect may include Severe allergic reactions (rash; hives; itching; difficulty breathing.
Useful Link	http://reference.medscape.com/drug/angiomax-angiox-bivalirudin-342137
PubMed ID	17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure	Th1006 (View) or (Download)

(2) Primary information
Entry 2
ID	1033
ThPP ID	Th1006
Therapeutic Peptide/Protein Name	Bivalirudin
Sequence	FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification	Ia
Molecular Weight	2180.2853
Chemical Formula	C98H138N24O33
Isoelectric Point	3.91
Hydrophobicity	-0.985
Melting Point (℃)	N.A.
Half Life	Creatinine clearance 10-29mL/min: 0.95 hours
Description	Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease	For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics	Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action	Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity	Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism	80% proteolytic cleavage
Absorption	Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution	0.2L/kg
Clearance	3.4 mL/min/kg [mild renal function]
Categories	Antithrombins
Patents Number	US5196404
Date of Issue	23/05/93
Date of Expiry	23/05/10
Drug Interaction	Gemcitabine, Gemcitabine may enhance the adverse/toxic effect of Bleomycin. The risk of pulmonary toxicity may be increased. Use extreme caution if using gemcitabine and bleomycin in combination. Monitor for the development of pulmonary toxicity
Target	N.A.
Information of corresponding available drug in the market
Brand Name	Angiox
Company	The Medicines Company UK Ltd
Brand Discription	N.A.
Prescribed for	Used as an anticoagulant in adult patients undergoing percutaneous coronary intervention (PCI), including patients with ST-segment elevation myocardial infarction (STEMI) undergoing primary PCI. Angiox is also indicated for the treatment of adult patients
Chemical Name	N.A.
Formulation	Each vial contains 250 mg bivalirudin.
Physcial Appearance	Powder for concentrated solution
Route of Administration	Injection
Recommended Dosage	0.75 mg/kg IV bolus, initially, followed by continuous infusion at rate of 1.75 mg/kg/hr for duration of procedure
Contraindication	Hypersensitivity, active bleeding or increased risk of bleeding because of haemostasis disorder or irreversible coagulation disorder, uncontrolled hypertension, subacute bacterial endocarditis, severe renal impairment and in dialysis dependent pateints,
Side Effects	N.A.
Useful Link	http://www.rxlist.com/angiomax-drug.htm
PubMed ID	17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure	Th1006 (View) or (Download)

(3) Primary information
Entry 3
ID	1034
ThPP ID	Th1006
Therapeutic Peptide/Protein Name	Bivalirudin
Sequence	FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification	Ia
Molecular Weight	2180.2853
Chemical Formula	C98H138N24O33
Isoelectric Point	3.91
Hydrophobicity	-0.985
Melting Point (℃)	N.A.
Half Life	Dialysis-dependant patients: 3.5 hours
Description	Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease	For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics	Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action	Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity	Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism	80% proteolytic cleavage
Absorption	Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution	0.2L/kg
Clearance	2.7 mL/min/kg [moderate renal function]
Categories	Antithrombins
Patents Number	CA2065150
Date of Issue	14/12/99
Date of Expiry	17/08/10
Drug Interaction	Ginkgo biloba, Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
Target	N.A.
Information of corresponding available drug in the market
Brand Name	N.A.
Company	N.A.
Brand Discription	N.A.
Prescribed for	N.A.
Chemical Name	N.A.
Formulation	N.A.
Physcial Appearance	N.A.
Route of Administration	N.A.
Recommended Dosage	N.A.
Contraindication	N.A.
Side Effects	N.A.
Useful Link	https://www.medicines.org.uk/emc/medicine/16741
PubMed ID	17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure	Th1006 (View) or (Download)

(4) Primary information
Entry 4
ID	1035
ThPP ID	Th1006
Therapeutic Peptide/Protein Name	Bivalirudin
Sequence	FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification	Ia
Molecular Weight	2180.2853
Chemical Formula	C98H138N24O33
Isoelectric Point	3.91
Hydrophobicity	-0.985
Melting Point (℃)	N.A.
Half Life	N.A.
Description	Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease	For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics	Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action	Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity	Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism	80% proteolytic cleavage
Absorption	Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution	0.2L/kg
Clearance	2.8 mL/min/kg [severe renal function]
Categories	Antithrombins
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	Rivaroxaban, Anticoagulants may enhance the anticoagulant effect of rivaroxaban. Avoid concurrent use of rivaroxaban with other anticoagulants whenever possible, other than during transition periods, due to the possible increased for bleeding.
Target	N.A.
Information of corresponding available drug in the market
Brand Name	N.A.
Company	N.A.
Brand Discription	N.A.
Prescribed for	N.A.
Chemical Name	N.A.
Formulation	N.A.
Physcial Appearance	N.A.
Route of Administration	N.A.
Recommended Dosage	N.A.
Contraindication	N.A.
Side Effects	N.A.
Useful Link	http://www.drugs.com/cdi/angiomax.html
PubMed ID	17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure	Th1006 (View) or (Download)

(5) Primary information
Entry 5
ID	1036
ThPP ID	Th1006
Therapeutic Peptide/Protein Name	Bivalirudin
Sequence	FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification	Ia
Molecular Weight	2180.2853
Chemical Formula	C98H138N24O33
Isoelectric Point	3.91
Hydrophobicity	-0.985
Melting Point (℃)	N.A.
Half Life	N.A.
Description	Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease	For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics	Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action	Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity	Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism	80% proteolytic cleavage
Absorption	Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution	0.2L/kg
Clearance	1 mL/min/kg [Dialysis-dependent patients]
Categories	Antithrombins
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	Treprostinil, The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Bivalirudin. Monitor for increased bleeding during concomitant thearpy.
Target	N.A.
Information of corresponding available drug in the market
Brand Name	N.A.
Company	N.A.
Brand Discription	N.A.
Prescribed for	N.A.
Chemical Name	N.A.
Formulation	N.A.
Physcial Appearance	N.A.
Route of Administration	N.A.
Recommended Dosage	N.A.
Contraindication	N.A.
Side Effects	N.A.
Useful Link	http://www.angiomax.com/
PubMed ID	17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure	Th1006 (View) or (Download)

(6) Primary information
Entry 6
ID	1037
ThPP ID	Th1006
Therapeutic Peptide/Protein Name	Bivalirudin
Sequence	FPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional Classification	Ia
Molecular Weight	2180.2853
Chemical Formula	C98H138N24O33
Isoelectric Point	3.91
Hydrophobicity	-0.985
Melting Point (℃)	N.A.
Half Life	N.A.
Description	Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/Disease	For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
Pharmacodynamics	Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of Action	Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
Toxicity	Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism	80% proteolytic cleavage
Absorption	Bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 Â± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution	0.2L/kg
Clearance	N.A.
Categories	Antithrombins
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	N.A.
Target	N.A.
Information of corresponding available drug in the market
Brand Name	N.A.
Company	N.A.
Brand Discription	N.A.
Prescribed for	N.A.
Chemical Name	N.A.
Formulation	N.A.
Physcial Appearance	N.A.
Route of Administration	N.A.
Recommended Dosage	N.A.
Contraindication	N.A.
Side Effects	N.A.
Useful Link	N.A.
PubMed ID	17381384, 16553503, 16466327, 12851152, 11156732
3-D Structure	Th1006 (View) or (Download)