Overview
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
Ramucirumab is indicated for the treatment of advanced or metastatic gastric or gastro-esophageal junction adenocarcinoma as a single agent or in combination with paclitaxel for patients who progress after prior fluoropyrimidine- or platinum-containing chemotherapy. It is indicated, in combination with erlotinib, for the first-line treatment of metastatic non-small cell lung cancer with epidermal growth factor exon 19 deletions or exon 21 (L858R) point mutations. It is also indicated in combination with docetaxel for the treatment of metastatic non-small cell lung cancer in patients who have progressed following prior platinum-based chemotherapy. Patients who have EGFR or ALK genomic aberrations should also have disease progression following FDA-approved therapy for these aberrations. Ramucirumab, in combination with FOLFIRI (folinic acid, fluorouracil, and irinotecan), is indicated for the treatment of metastatic colorectal cancer in patients who have progressed following therapy with bevacizumab, oxaliplatin, and a fluoropyrimidine. Lastly, ramucirumab is indicated for the treatment of hepatocellular carcinoma in patients with an alpha-fetoprotein level ≥400 ng/mL and have previously been treated with sorafenib.
Associated Conditions
- Advanced Gastric or Gastroesophageal Junction Adenocarcinoma
- Hepatocellular Carcinoma
- Metastatic Colorectal Cancer (CRC)
- Metastatic Non-Small Cell Lung Cancer
- Metastatic Gastric or Gastroesophageal Junction (GEJ) Adenocarcinoma
Research Report
A Comprehensive Monograph on Ramucirumab (Cyramza): Pharmacology, Clinical Efficacy, and Therapeutic Role in Oncology
Section 1: Executive Summary & Drug Profile
1.1. Overview
Ramucirumab, marketed under the brand name Cyramza®, is a fully human immunoglobulin G1 (IgG1) monoclonal antibody that functions as a direct and specific antagonist of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2).[1] By selectively targeting this key receptor, ramucirumab inhibits tumor angiogenesis—the formation of new blood vessels that are essential for tumor growth, survival, and metastasis.[4] This mechanism of action has established ramucirumab as an important therapeutic agent in the treatment of several advanced or metastatic solid tumors. It has secured regulatory approvals for use in gastric and gastroesophageal junction (GEJ) adenocarcinoma, non-small cell lung cancer (NSCLC), metastatic colorectal cancer (mCRC), and a biomarker-defined subpopulation of hepatocellular carcinoma (HCC).[2]
Clinical Trials
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Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2023/07/03 | Phase 1 | Not yet recruiting | National Health Research Institutes, Taiwan | ||
2023/05/12 | Phase 1 | Recruiting | |||
2023/04/05 | Phase 1 | Completed | |||
2022/12/08 | Phase 2 | Recruiting | |||
2022/12/01 | Phase 3 | Active, not recruiting | |||
2022/05/09 | Phase 1 | Recruiting | |||
2022/04/05 | Phase 2 | Terminated | |||
2021/10/27 | Phase 2 | Active, not recruiting | |||
2021/10/07 | Phase 2 | Terminated | |||
2021/09/30 | Phase 1 | Terminated |
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