Detailed description page of THPdb

Details of Th1199 which contains 1 entries.

Entry 1
(1) Primary information
ID 1805
ThPP ID Th1199
Therapeutic Peptide/Protein Name Ramucirumab
Sequence HINGE-REGION(215-229) EVQLVQSGGGLVKPGGSLRLSCAASGFT view full sequnce in fasta
Functional Classification IIIc
Molecular Weight 143600
Chemical Formula C6374H9864N1692O1996S46
Isoelectric Point NA
Hydrophobicity NA
Melting Point (℃) NA
Half Life 15 days
Description Ramucirumab is a human monoclonal antibody (IgG1) against vascular endothelial growth factor receptor 2 (VEGFR2), a type II trans-membrane tyrosine kinase receptor expressed on endothelial cells. By binding to VEGFR2, ramucirumab prevents binding of its ligands (VEGF-A, VEGF-C, and VEGF-D), thereby preventing VEGF-stimulated receptor phosphorylation and downstream ligand-induced proliferation, permeability, and migration of human endothelial cells. VEGFR stimulation also mediates downstream signalling required for angiogenesis and is postulated to be heavily involved in cancer progression, making it a highly likely drug target. In contrast to other agents directed against VEGFR-2, ramucirumab binds a specific epitope on the extracellular domain of VEGFR-2, thereby blocking all VEGF ligands from binding to it. Ramucirumab is indicated for us in advanced gastric or gastro-esophageal junction adenocarcinoma as a single agent or in combination with paclitaxel after prior fluoropyrimidine- or platinum-containing chemotherapy.
Indication/Disease For use in advanced gastric or gastro-esophageal junction adenocarcinoma as a single agent or in combination with paclitaxel after prior fluoropyrimidine- or platinum-containing chemotherapy.
Pharmacodynamics Ramucirumab inhibits ligandstimulated activation of VEGF Receptor 2, thereby inhibiting ligand-induced proliferation, and migration of human endothelial cells. Ramucirumab inhibited angiogenesis in an in vivo animal model.
Mechanism of Action Ramucirumab is a human monoclonal antibody (IgG1) against vascular endothelial growth factor receptor 2 (VEGFR2), a type II trans-membrane tyrosine kinase receptor expressed on endothelial cells. By binding to VEGFR2, ramucirumab prevents binding of its ligands (VEGF-A, VEGF-C, and VEGF-D), thereby preventing VEGF-stimulated receptor phosphorylation and downstream ligand-induced proliferation, permeability, and migration of human endothelial cells.
Toxicity Ramucirumab packaging includes warnings for arterial thromboembolic events, hypertension, infusion-related reactions, gastrointestinal perforation, clinical deterioration in patients with cirrhosis, and reversible posterior leukoencephalopathy syndrome. The most common reactions observed in single-agent-treated patients at a rate of >10% and >2% higher than placebo were hypertension and diarrhea. The most common adverse reactions observed in patients treated with ramucirumab plus paclitaxel at a rate of of >30% and >2% higher than placebo plus paclitaxel were fatigue, neutropenia, diarrhea, and epistaxis.
Metabolism
Absorption
Volume of Distribution 5.5 L
Clearance 0.014 L/hour
Categories Antineoplastic and Immunomodulating Agents
Patents Number US2013067098
Date of Issue 40849
Date of Expiry 48154
Drug Interaction Belimumab, Pamidronate
Target Vascular endothelial growth factor receptor 2
Information of corresponding available drug in the market
Brand Name Cyramza
Company Eli Lilly and Company
Brand Discription CYRAMZA (ramucirumab) is a recombinant human IgG1 monoclonal antibody that specifically binds to vascular endothelial growth factor receptor 2. CYRAMZA has an approximate molecular weight of 147 kDa. CYRAMZA is produced in genetically engineered mammalian NS0 cells.
Prescribed for CYRAMZAÂ®as a single agent, or in combination with paclitaxel, is indicated for the treatment of patients with advanced or metastatic, gastric or gastro-esophageal junction adenocarcinoma with disease progression on or after prior fluoropyrimidine-or platinum-containing chemotherapy.
Chemical Name NA
Formulation 10 mg/mL
Physcial Appearance Solution
Route of Administration Intravenous
Recommended Dosage Either 8mg/kg or 10 mg/kg every 2 weeks
Contraindication NA
Side Effects Hemorrhage; Arterial Thromboembolic Events; Hypertension; Infusion-Related Reactions; Gastrointestinal Perforation; Impaired Wound Healing; Patients with Child-Pugh B or C Cirrhosis; Reversible Posterior Leukoencephalopathy Syndrome; Proteinuria Including Nephrotic Syndrome; Thyroid Dysfunction.
Useful Link http://www.rxlist.com/cyramza-drug.htm
PubMed ID 28285368, 28277882, 28276858, 28260227, 28220199, 28220020, 28212372, 28203696, 28203161
3-D Structure Th1199 Heavy chianor (Download)Th1199 Light chian (View) or (Download)

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

(1) Primary information
Entry 1
ID	1805
ThPP ID	Th1199
Therapeutic Peptide/Protein Name	Ramucirumab
Sequence	HINGE-REGION(215-229) EVQLVQSGGGLVKPGGSLRLSCAASGFT view full sequnce in fasta
Functional Classification	IIIc
Molecular Weight	143600
Chemical Formula	C6374H9864N1692O1996S46
Isoelectric Point	NA
Hydrophobicity	NA
Melting Point (℃)	NA
Half Life	15 days
Description	Ramucirumab is a human monoclonal antibody (IgG1) against vascular endothelial growth factor receptor 2 (VEGFR2), a type II trans-membrane tyrosine kinase receptor expressed on endothelial cells. By binding to VEGFR2, ramucirumab prevents binding of its ligands (VEGF-A, VEGF-C, and VEGF-D), thereby preventing VEGF-stimulated receptor phosphorylation and downstream ligand-induced proliferation, permeability, and migration of human endothelial cells. VEGFR stimulation also mediates downstream signalling required for angiogenesis and is postulated to be heavily involved in cancer progression, making it a highly likely drug target. In contrast to other agents directed against VEGFR-2, ramucirumab binds a specific epitope on the extracellular domain of VEGFR-2, thereby blocking all VEGF ligands from binding to it. Ramucirumab is indicated for us in advanced gastric or gastro-esophageal junction adenocarcinoma as a single agent or in combination with paclitaxel after prior fluoropyrimidine- or platinum-containing chemotherapy.
Indication/Disease	For use in advanced gastric or gastro-esophageal junction adenocarcinoma as a single agent or in combination with paclitaxel after prior fluoropyrimidine- or platinum-containing chemotherapy.
Pharmacodynamics	Ramucirumab inhibits ligandstimulated activation of VEGF Receptor 2, thereby inhibiting ligand-induced proliferation, and migration of human endothelial cells. Ramucirumab inhibited angiogenesis in an in vivo animal model.
Mechanism of Action	Ramucirumab is a human monoclonal antibody (IgG1) against vascular endothelial growth factor receptor 2 (VEGFR2), a type II trans-membrane tyrosine kinase receptor expressed on endothelial cells. By binding to VEGFR2, ramucirumab prevents binding of its ligands (VEGF-A, VEGF-C, and VEGF-D), thereby preventing VEGF-stimulated receptor phosphorylation and downstream ligand-induced proliferation, permeability, and migration of human endothelial cells.
Toxicity	Ramucirumab packaging includes warnings for arterial thromboembolic events, hypertension, infusion-related reactions, gastrointestinal perforation, clinical deterioration in patients with cirrhosis, and reversible posterior leukoencephalopathy syndrome. The most common reactions observed in single-agent-treated patients at a rate of >10% and >2% higher than placebo were hypertension and diarrhea. The most common adverse reactions observed in patients treated with ramucirumab plus paclitaxel at a rate of of >30% and >2% higher than placebo plus paclitaxel were fatigue, neutropenia, diarrhea, and epistaxis.
Metabolism
Absorption
Volume of Distribution	5.5 L
Clearance	0.014 L/hour
Categories	Antineoplastic and Immunomodulating Agents
Patents Number	US2013067098
Date of Issue	40849
Date of Expiry	48154
Drug Interaction	Belimumab, Pamidronate
Target	Vascular endothelial growth factor receptor 2
Information of corresponding available drug in the market
Brand Name	Cyramza
Company	Eli Lilly and Company
Brand Discription	CYRAMZA (ramucirumab) is a recombinant human IgG1 monoclonal antibody that specifically binds to vascular endothelial growth factor receptor 2. CYRAMZA has an approximate molecular weight of 147 kDa. CYRAMZA is produced in genetically engineered mammalian NS0 cells.
Prescribed for	CYRAMZAÂ®as a single agent, or in combination with paclitaxel, is indicated for the treatment of patients with advanced or metastatic, gastric or gastro-esophageal junction adenocarcinoma with disease progression on or after prior fluoropyrimidine-or platinum-containing chemotherapy.
Chemical Name	NA
Formulation	10 mg/mL
Physcial Appearance	Solution
Route of Administration	Intravenous
Recommended Dosage	Either 8mg/kg or 10 mg/kg every 2 weeks
Contraindication	NA
Side Effects	Hemorrhage; Arterial Thromboembolic Events; Hypertension; Infusion-Related Reactions; Gastrointestinal Perforation; Impaired Wound Healing; Patients with Child-Pugh B or C Cirrhosis; Reversible Posterior Leukoencephalopathy Syndrome; Proteinuria Including Nephrotic Syndrome; Thyroid Dysfunction.
Useful Link	http://www.rxlist.com/cyramza-drug.htm
PubMed ID	28285368, 28277882, 28276858, 28260227, 28220199, 28220020, 28212372, 28203696, 28203161
3-D Structure	Th1199 Heavy chianor (Download)Th1199 Light chian (View) or (Download)