Rivoceranib API, commonly supplied in its mesylate salt form as Rivoceranib Mesylate, is a small-molecule receptor tyrosine kinase inhibitor with anti-angiogenic activity. Rivoceranib is also known by the development code YN968D1 and the name Apatinib, while the pharmaceutical salt is known as Apatinib Mesylate. FDA substance records identify Rivoceranib Mesylate as the 1:1 methanesulfonate salt of rivoceranib.
Rivoceranib primarily inhibits vascular endothelial growth factor receptor 2 (VEGFR-2/KDR), thereby interfering with VEGF-mediated signaling involved in endothelial-cell proliferation, migration and tumor angiogenesis. It also demonstrates activity against other kinase targets, including c-KIT and RET.
Rivoceranib Mesylate is a chemically defined small-molecule pharmaceutical ingredient. The API is associated with the CAS number 1218779-75-9, while the rivoceranib free base is separately identified as CAS 811803-05-1. FDA GSRS assigns UNII TK02X14ASJ to Rivoceranib Mesylate and 5S371K6132 to Rivoceranib.
The mesylate salt has a molecular weight of approximately 493.6 g/mol. It is achiral and has no defined stereocenters.
Rivoceranib Mesylate is the methanesulfonate salt of rivoceranib. The molecule contains pyridine-based structural elements together with a substituted cyclopentyl nitrile group and a carboxamide functionality. Its pharmaceutical activity is associated principally with inhibition of VEGFR-2 signaling.
The compound can exist in different crystalline forms. Published patent literature describes multiple rivoceranib and rivoceranib mesylate polymorphs, making solid-state characterization important during API development and quality control.
Rivoceranib is investigated and developed primarily as an anti-neoplastic and anti-angiogenic agent. Its principal pharmacological target is VEGFR-2, making it relevant to oncology applications in which VEGF-driven angiogenesis contributes to tumor growth.
Rivoceranib mesylate has been investigated across several solid-tumor indications, including gastric cancer, hepatocellular carcinoma and other oncology settings. The European Medicines Agency has also granted orphan designation for rivoceranib mesilate in hepatocellular carcinoma; orphan designation itself does not constitute marketing authorization.
Quality evaluation of Rivoceranib API should address chemical identity, assay/purity, related substances, residual solvents, water or loss on drying, inorganic residues and solid-state characteristics as applicable to the manufacturer's validated specification.
Typical analytical approaches include HPLC/UPLC for assay and related substances, LC-MS for molecular confirmation, NMR for structural identity, IR spectroscopy, water/LOD testing, elemental or inorganic residue testing and XRPD/DSC for solid-state characterization.
Because rivoceranib mesylate has documented polymorphic forms, XRPD and thermal analysis can be important when a particular crystalline form is part of the API control strategy.
A reliable Rivoceranib API manufacturing program should maintain controlled synthesis, purification and crystallization processes together with validated analytical methods. Particular attention should be given to chemical purity, related substances, residual solvents and crystalline-form control.
The API can be supplied with appropriate quality documentation such as Certificate of Analysis, analytical methods, specifications, safety documentation and technical documentation according to the applicable customer and regulatory requirements.
Rivoceranib Mesylate should be packaged in a suitable well-closed, moisture-protective pharmaceutical container appropriate for the material and its validated stability profile.
Commercial research-grade material is commonly stored under controlled, dry conditions; one current analytical certificate specifies short-term storage at 0–4°C and long-term storage at −20°C. These temperatures should be treated as that supplier's storage recommendation rather than a universal pharmacopoeial requirement.
Typical API documentation may include:
Rivoceranib Mesylate is a well-characterized small-molecule VEGFR-2 inhibitor with established chemical identity and extensive pharmaceutical-development literature. Its defined molecular structure, documented salt form and recognized importance of polymorph control make comprehensive analytical characterization particularly important for API quality.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Melting Point | 193.5–195°C |