Detailed description page of THPdb

Details of Th1088 which contains 3 entries.

Entry 1
(1) Primary information
ID 1462
ThPP ID Th1088
Therapeutic Peptide/Protein Name Enfuvirtide
Sequence YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF view full sequnce in fasta
Functional Classification IIa
Molecular Weight 4491.876
Chemical Formula C204H301N51O64
Isoelectric Point 4.3
Hydrophobicity -0.875
Melting Point (℃) N.A.
Half Life 3.8 Â± 0.6 hrs
Description 36 residue, synthetically prepared peptide with N-terminal acetylation and C-terminal amidation. It blocks the fusion of HIV-1 with CD4 cells.
Indication/Disease Enfuvirtide is an antiretroviral drug used in combination therapy for the treatment of HIV-1/AIDS.
Pharmacodynamics N.A.
Mechanism of Action Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. It works by disrupting the HIV-1 molecular machinery at the final stage of fusion with the target cell, preventing uninfected cells from becoming infected. Enfuvirtide is a biomimetic peptide that was rationally designed to mimic components of the HIV-1 fusion machinery and displace them, preventing normal fusion.
Toxicity N.A.
Metabolism Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.
Absorption After a 90 mg single subcutaneous injection of Enfuvirtide into the abdomen in 12 HIV-1 infected subjects, the mean peak concentration is 4.59Â±1.5 ug/ml and the median time to peak concentration was 8 hours (ranged from 3 to12 hours).
Volume of Distribution 5.5 Â± 1.1 L
Clearance 24.8 Â± 4.1 mL/h/kg [HIV-1 infected adult and pediatric subjects following a 90-mg single SC dose of enfuvirtide] 30.6 Â± 10.6 mL/h/kg [Following 90-mg twice daily dosing of FUZEON SC in combination with other antiretroviral agents in HIV-1 infected subjects] 40 Â± 17 mL/h/kg [pediatric patients in the presence of concomitant medications including antiretroviral agents receiving the 2 mg/kg twice daily dose]
Categories HIV Fusion Inhibitors
Patents Number US6475491
Date of Issue 08/06/99
Date of Expiry 08/06/19
Drug Interaction N.A.
Target N.A.
Information of corresponding available drug in the market
Brand Name FUZEON
Company Trimeris, Roche
Brand Discription FUZEON (enfuvirtide) is an inhibitor of the fusion of HIV-1 with CD4 cells. Enfuvirtide is a linear 36-amino acid synthetic peptide with the N-terminus acetylated and the C-terminus is a carboxamide. It is composed of naturally occurring L-amino acid residues. Enfuvirtide is a white to off-white amorphous solid. It has negligible solubility in pure water and the solubility increases in aqueous buffers (pH 7.5) to 85-142 g/100 mL. The empirical formula of enfuvirtide is C204H301N51O64, and the molecular weight is 4492
Prescribed for FUZEON in combination with other antiretroviral agents is indicated for the treatment of HIV-1 infection in treatment experienced patients with evidence of HIV-1 replication despite ongoing antiretroviral therapy.
Chemical Name N.A.
Formulation Each single-use vial contains 108 mg of enfuvirtide for the delivery of 90 mg. Prior to subcutaneous administration, the contents of the vial are reconstituted with 1.1 mL of Sterile Water for Injection giving a volume of approximately 1.2 mL to provide the delivery of 1 mL of the solution. Each 1 mL of the reconstituted solution contains approximately 90 mg of enfuvirtide with approximate amounts of the following excipients: 22.55 mg of mannitol, 2.39 mg of sodium carbonate (anhydrous), and sodium hydroxide and hydrochloric acid for pH adjustment as needed. The reconstituted solution has an approximate pH of 9.0
Physcial Appearance White to off-white, sterile, lyophilized powder. Each single-use vial contains 108 mg of enfuvirtide for the delivery of 90 mg. Prior to subcutaneous administration, the contents of the vial are reconstituted with 1.1 mL of Sterile Water for Injection giving a volume of approximately 1.2 mL to provi
Route of Administration Subcutaneous
Recommended Dosage 90 mg (1 mL) twice daily injected subcutaneously into the upper arm, anterior thigh or abdomen. Each injection should be given at a site different from the preceding injection site, and only where there is no current injection site reaction from an earlier dose.
Contraindication FUZEON is contraindicated in patients with known hypersensitivity to FUZEON or any of its components
Side Effects fever, chills, chest congestion, cough with yellow or green mucus, stabbing chest pain, wheezing, feeling short of breath; signs of a new infection such as sore throat, flu symptoms, swollen glands, easy bruising or bleeding.
Useful Link http://www.rxlist.com/fuzeon-drug.htm http://www.drugs.com/mtm/enfuvirtide.html
PubMed ID 25594223, 25553058, 24966037, 24816213, 24616600, 24500189, 24446896, 24366751
3-D Structure Th1088 (View) or (Download)

Entry 2
(2) Primary information
ID 1463
ThPP ID Th1088
Therapeutic Peptide/Protein Name Enfuvirtide
Sequence YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF view full sequnce in fasta
Functional Classification IIa
Molecular Weight 4491.876
Chemical Formula C204H301N51O64
Isoelectric Point 4.3
Hydrophobicity -0.875
Melting Point (℃) N.A.
Half Life 3.8 Â± 0.6 hrs
Description 36 residue, synthetically prepared peptide with N-terminal acetylation and C-terminal amidation. It blocks the fusion of HIV-1 with CD4 cells.
Indication/Disease Enfuvirtide is an antiretroviral drug used in combination therapy for the treatment of HIV-1/AIDS.
Pharmacodynamics N.A.
Mechanism of Action Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. It works by disrupting the HIV-1 molecular machinery at the final stage of fusion with the target cell, preventing uninfected cells from becoming infected. Enfuvirtide is a biomimetic peptide that was rationally designed to mimic components of the HIV-1 fusion machinery and displace them, preventing normal fusion.
Toxicity N.A.
Metabolism Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.
Absorption After a 90 mg single subcutaneous injection of Enfuvirtide into the abdomen in 12 HIV-1 infected subjects, the mean peak concentration is 4.59Â±1.5 ug/ml and the median time to peak concentration was 8 hours (ranged from 3 to12 hours).
Volume of Distribution 5.5 Â± 1.1 L
Clearance 24.8 Â± 4.1 mL/h/kg [HIV-1 infected adult and pediatric subjects following a 90-mg single SC dose of enfuvirtide] 30.6 Â± 10.6 mL/h/kg [Following 90-mg twice daily dosing of FUZEON SC in combination with other antiretroviral agents in HIV-1 infected subjects] 40 Â± 17 mL/h/kg [pediatric patients in the presence of concomitant medications including antiretroviral agents receiving the 2 mg/kg twice daily dose]
Categories HIV Fusion Inhibitors
Patents Number US5464933
Date of Issue 08/06/97
Date of Expiry 08/06/17
Drug Interaction N.A.
Target Oxytocin receptor,Oxytocin-neurophysin 1
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 25594223, 25553058, 24966037, 24816213, 24616600, 24500189, 24446896, 24366751
3-D Structure Th1088 (View) or (Download)

Entry 3
(3) Primary information
ID 1464
ThPP ID Th1088
Therapeutic Peptide/Protein Name Enfuvirtide
Sequence YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF view full sequnce in fasta
Functional Classification IIa
Molecular Weight 4491.876
Chemical Formula C204H301N51O64
Isoelectric Point 4.3
Hydrophobicity -0.875
Melting Point (℃) N.A.
Half Life 3.8 Â± 0.6 hrs
Description 36 residue, synthetically prepared peptide with N-terminal acetylation and C-terminal amidation. It blocks the fusion of HIV-1 with CD4 cells.
Indication/Disease Enfuvirtide is an antiretroviral drug used in combination therapy for the treatment of HIV-1/AIDS.
Pharmacodynamics N.A.
Mechanism of Action Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. It works by disrupting the HIV-1 molecular machinery at the final stage of fusion with the target cell, preventing uninfected cells from becoming infected. Enfuvirtide is a biomimetic peptide that was rationally designed to mimic components of the HIV-1 fusion machinery and displace them, preventing normal fusion.
Toxicity N.A.
Metabolism Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.
Absorption After a 90 mg single subcutaneous injection of Enfuvirtide into the abdomen in 12 HIV-1 infected subjects, the mean peak concentration is 4.59Â±1.5 ug/ml and the median time to peak concentration was 8 hours (ranged from 3 to12 hours).
Volume of Distribution 5.5 Â± 1.1 L
Clearance 24.8 Â± 4.1 mL/h/kg [HIV-1 infected adult and pediatric subjects following a 90-mg single SC dose of enfuvirtide] 30.6 Â± 10.6 mL/h/kg [Following 90-mg twice daily dosing of FUZEON SC in combination with other antiretroviral agents in HIV-1 infected subjects] 40 Â± 17 mL/h/kg [pediatric patients in the presence of concomitant medications including antiretroviral agents receiving the 2 mg/kg twice daily dose]
Categories HIV Fusion Inhibitors
Patents Number CA2224008
Date of Issue 19/08/13
Date of Expiry 07/06/20
Drug Interaction N.A.
Target Envelope glycoprotein
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 25594223, 25553058, 24966037, 24816213, 24616600, 24500189, 24446896, 24366751
3-D Structure Th1088 (View) or (Download)

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

(1) Primary information
Entry 1
ID	1462
ThPP ID	Th1088
Therapeutic Peptide/Protein Name	Enfuvirtide
Sequence	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	4491.876
Chemical Formula	C204H301N51O64
Isoelectric Point	4.3
Hydrophobicity	-0.875
Melting Point (℃)	N.A.
Half Life	3.8 Â± 0.6 hrs
Description	36 residue, synthetically prepared peptide with N-terminal acetylation and C-terminal amidation. It blocks the fusion of HIV-1 with CD4 cells.
Indication/Disease	Enfuvirtide is an antiretroviral drug used in combination therapy for the treatment of HIV-1/AIDS.
Pharmacodynamics	N.A.
Mechanism of Action	Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. It works by disrupting the HIV-1 molecular machinery at the final stage of fusion with the target cell, preventing uninfected cells from becoming infected. Enfuvirtide is a biomimetic peptide that was rationally designed to mimic components of the HIV-1 fusion machinery and displace them, preventing normal fusion.
Toxicity	N.A.
Metabolism	Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.
Absorption	After a 90 mg single subcutaneous injection of Enfuvirtide into the abdomen in 12 HIV-1 infected subjects, the mean peak concentration is 4.59Â±1.5 ug/ml and the median time to peak concentration was 8 hours (ranged from 3 to12 hours).
Volume of Distribution	5.5 Â± 1.1 L
Clearance	24.8 Â± 4.1 mL/h/kg [HIV-1 infected adult and pediatric subjects following a 90-mg single SC dose of enfuvirtide] 30.6 Â± 10.6 mL/h/kg [Following 90-mg twice daily dosing of FUZEON SC in combination with other antiretroviral agents in HIV-1 infected subjects] 40 Â± 17 mL/h/kg [pediatric patients in the presence of concomitant medications including antiretroviral agents receiving the 2 mg/kg twice daily dose]
Categories	HIV Fusion Inhibitors
Patents Number	US6475491
Date of Issue	08/06/99
Date of Expiry	08/06/19
Drug Interaction	N.A.
Target	N.A.
Information of corresponding available drug in the market
Brand Name	FUZEON
Company	Trimeris, Roche
Brand Discription	FUZEON (enfuvirtide) is an inhibitor of the fusion of HIV-1 with CD4 cells. Enfuvirtide is a linear 36-amino acid synthetic peptide with the N-terminus acetylated and the C-terminus is a carboxamide. It is composed of naturally occurring L-amino acid residues. Enfuvirtide is a white to off-white amorphous solid. It has negligible solubility in pure water and the solubility increases in aqueous buffers (pH 7.5) to 85-142 g/100 mL. The empirical formula of enfuvirtide is C204H301N51O64, and the molecular weight is 4492
Prescribed for	FUZEON in combination with other antiretroviral agents is indicated for the treatment of HIV-1 infection in treatment experienced patients with evidence of HIV-1 replication despite ongoing antiretroviral therapy.
Chemical Name	N.A.
Formulation	Each single-use vial contains 108 mg of enfuvirtide for the delivery of 90 mg. Prior to subcutaneous administration, the contents of the vial are reconstituted with 1.1 mL of Sterile Water for Injection giving a volume of approximately 1.2 mL to provide the delivery of 1 mL of the solution. Each 1 mL of the reconstituted solution contains approximately 90 mg of enfuvirtide with approximate amounts of the following excipients: 22.55 mg of mannitol, 2.39 mg of sodium carbonate (anhydrous), and sodium hydroxide and hydrochloric acid for pH adjustment as needed. The reconstituted solution has an approximate pH of 9.0
Physcial Appearance	White to off-white, sterile, lyophilized powder. Each single-use vial contains 108 mg of enfuvirtide for the delivery of 90 mg. Prior to subcutaneous administration, the contents of the vial are reconstituted with 1.1 mL of Sterile Water for Injection giving a volume of approximately 1.2 mL to provi
Route of Administration	Subcutaneous
Recommended Dosage	90 mg (1 mL) twice daily injected subcutaneously into the upper arm, anterior thigh or abdomen. Each injection should be given at a site different from the preceding injection site, and only where there is no current injection site reaction from an earlier dose.
Contraindication	FUZEON is contraindicated in patients with known hypersensitivity to FUZEON or any of its components
Side Effects	fever, chills, chest congestion, cough with yellow or green mucus, stabbing chest pain, wheezing, feeling short of breath; signs of a new infection such as sore throat, flu symptoms, swollen glands, easy bruising or bleeding.
Useful Link	http://www.rxlist.com/fuzeon-drug.htm http://www.drugs.com/mtm/enfuvirtide.html
PubMed ID	25594223, 25553058, 24966037, 24816213, 24616600, 24500189, 24446896, 24366751
3-D Structure	Th1088 (View) or (Download)

(2) Primary information
Entry 2
ID	1463
ThPP ID	Th1088
Therapeutic Peptide/Protein Name	Enfuvirtide
Sequence	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	4491.876
Chemical Formula	C204H301N51O64
Isoelectric Point	4.3
Hydrophobicity	-0.875
Melting Point (℃)	N.A.
Half Life	3.8 Â± 0.6 hrs
Description	36 residue, synthetically prepared peptide with N-terminal acetylation and C-terminal amidation. It blocks the fusion of HIV-1 with CD4 cells.
Indication/Disease	Enfuvirtide is an antiretroviral drug used in combination therapy for the treatment of HIV-1/AIDS.
Pharmacodynamics	N.A.
Mechanism of Action	Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. It works by disrupting the HIV-1 molecular machinery at the final stage of fusion with the target cell, preventing uninfected cells from becoming infected. Enfuvirtide is a biomimetic peptide that was rationally designed to mimic components of the HIV-1 fusion machinery and displace them, preventing normal fusion.
Toxicity	N.A.
Metabolism	Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.
Absorption	After a 90 mg single subcutaneous injection of Enfuvirtide into the abdomen in 12 HIV-1 infected subjects, the mean peak concentration is 4.59Â±1.5 ug/ml and the median time to peak concentration was 8 hours (ranged from 3 to12 hours).
Volume of Distribution	5.5 Â± 1.1 L
Clearance	24.8 Â± 4.1 mL/h/kg [HIV-1 infected adult and pediatric subjects following a 90-mg single SC dose of enfuvirtide] 30.6 Â± 10.6 mL/h/kg [Following 90-mg twice daily dosing of FUZEON SC in combination with other antiretroviral agents in HIV-1 infected subjects] 40 Â± 17 mL/h/kg [pediatric patients in the presence of concomitant medications including antiretroviral agents receiving the 2 mg/kg twice daily dose]
Categories	HIV Fusion Inhibitors
Patents Number	US5464933
Date of Issue	08/06/97
Date of Expiry	08/06/17
Drug Interaction	N.A.
Target	Oxytocin receptor,Oxytocin-neurophysin 1
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	25594223, 25553058, 24966037, 24816213, 24616600, 24500189, 24446896, 24366751
3-D Structure	Th1088 (View) or (Download)

(3) Primary information
Entry 3
ID	1464
ThPP ID	Th1088
Therapeutic Peptide/Protein Name	Enfuvirtide
Sequence	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	4491.876
Chemical Formula	C204H301N51O64
Isoelectric Point	4.3
Hydrophobicity	-0.875
Melting Point (℃)	N.A.
Half Life	3.8 Â± 0.6 hrs
Description	36 residue, synthetically prepared peptide with N-terminal acetylation and C-terminal amidation. It blocks the fusion of HIV-1 with CD4 cells.
Indication/Disease	Enfuvirtide is an antiretroviral drug used in combination therapy for the treatment of HIV-1/AIDS.
Pharmacodynamics	N.A.
Mechanism of Action	Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. It works by disrupting the HIV-1 molecular machinery at the final stage of fusion with the target cell, preventing uninfected cells from becoming infected. Enfuvirtide is a biomimetic peptide that was rationally designed to mimic components of the HIV-1 fusion machinery and displace them, preventing normal fusion.
Toxicity	N.A.
Metabolism	Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.
Absorption	After a 90 mg single subcutaneous injection of Enfuvirtide into the abdomen in 12 HIV-1 infected subjects, the mean peak concentration is 4.59Â±1.5 ug/ml and the median time to peak concentration was 8 hours (ranged from 3 to12 hours).
Volume of Distribution	5.5 Â± 1.1 L
Clearance	24.8 Â± 4.1 mL/h/kg [HIV-1 infected adult and pediatric subjects following a 90-mg single SC dose of enfuvirtide] 30.6 Â± 10.6 mL/h/kg [Following 90-mg twice daily dosing of FUZEON SC in combination with other antiretroviral agents in HIV-1 infected subjects] 40 Â± 17 mL/h/kg [pediatric patients in the presence of concomitant medications including antiretroviral agents receiving the 2 mg/kg twice daily dose]
Categories	HIV Fusion Inhibitors
Patents Number	CA2224008
Date of Issue	19/08/13
Date of Expiry	07/06/20
Drug Interaction	N.A.
Target	Envelope glycoprotein
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	25594223, 25553058, 24966037, 24816213, 24616600, 24500189, 24446896, 24366751
3-D Structure	Th1088 (View) or (Download)