==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

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1805 details
Primary information
ThPP IDTh1199
Therapeutic Peptide/Protein NameRamucirumab
SequenceHINGE-REGION(215-229) EVQLVQSGGGLVKPGGSLRLSCAASGFT view full sequnce in fasta
Functional ClassificationIIIc
Molecular Weight143600
Chemical FormulaC6374H9864N1692O1996S46
Isoelectric PointNA
HydrophobicityNA
Melting Point (℃)NA
Half Life15 days
DescriptionRamucirumab 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/DiseaseFor 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.
PharmacodynamicsRamucirumab 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 ActionRamucirumab 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.
ToxicityRamucirumab 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 Distribution5.5 L
Clearance0.014 L/hour
CategoriesAntineoplastic and Immunomodulating Agents
Patents NumberUS2013067098
Date of Issue40849
Date of Expiry48154
Drug InteractionBelimumab, Pamidronate
TargetVascular endothelial growth factor receptor 2
Information of corresponding available drug in the market
Brand NameCyramza
CompanyEli Lilly and Company
Brand DiscriptionCYRAMZA (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 forCYRAMZA®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 NameNA
Formulation10 mg/mL
Physcial AppearnceSolution
Route of AdministrationIntravenous
Recommended DosageEither 8mg/kg or 10 mg/kg every 2 weeks
ContraindicationNA
Side EffectsHemorrhage; 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 Linkhttp://www.rxlist.com/cyramza-drug.htm
PubMed ID28285368, 28277882, 28276858, 28260227, 28220199, 28220020, 28212372, 28203696, 28203161
3-D StructureTh1199 Heavy chianor (Download)Th1199 Light chian (View) or (Download)