Regorafenib, sold under the brand name Stivarga among others, is an oral multi-kinase inhibitor developed by Bayer which targets angiogenic, stromal and oncogenic receptor tyrosine kinase. Regorafenib shows anti-angiogenic activity due to its dual targete and additionally functions as an ATP-competitive small molecule that binds the kinase ATP-binding pocket to inhibit phosphorylation of VEGFR1-3 and TIE2 (angiogenesis), PDGFR and select FGFR isoforms (stromal signaling), and oncogenic kinases including KIT, RET and members of the RAF family (RAF1, BRAF) to suppress tumor-cell proliferation and survival; active circulating metabolites, primarily the N-oxide (M-2) and the N-desmethyl (M-5) species, contribute to overall pharmacologic activity and prolong pharmacodynamic effects.
Parent: Regorafenib
Parent: Regorafenib / Regorafenib Monohydrate
Parent: Regorafenib
Parent: Regorafenib
Parent: Regorafenib / Sorafenib
Typical API quality control and regulatory specifications for regorafenib describe limits for related substances and degradation products consistent with ICH guidance: individual specified related compounds are commonly limited in the range of 0.2 to 0.5 percent w/w, total impurities are typically controlled to not exceed about 1.0 percent w/w, and reporting thresholds for unknown impurities follow ICH Q3A/Q3B (for this class of small molecule impurities reporting thresholds may be in the low 0.05 percent range depending on maximum daily dose); genotoxic impurities are controlled to ICH M7-specified ppm levels. Common related compounds and degradants monitored by HPLC/LC-MS include the N-oxide (M-2), N-desmethyl (M-5), the combined N-desmethyl N-oxide, amide hydrolysis products, phenoxy ether cleavage products, dehalogenated or dealkylated analogs, and residual synthetic intermediates derived from the 4-chloro-3-(trifluoromethyl)phenyl and pyridine building blocks; residual solvents and elemental impurities must meet ICH Q3C and Q3D limits.
No. Regorafenib is a targeted small-molecule kinase inhibitor used as a form of systemic cancer therapy; it differs from traditional cytotoxic chemotherapy because it selectively inhibits specific signaling kinases involved in angiogenesis, stromal support and oncogenic signaling rather than nonselectively damaging DNA or all rapidly dividing cells.
Regorafenib binds to the ATP-binding pocket of multiple receptor and nonreceptor tyrosine kinases, blocking their catalytic activity and preventing downstream phosphorylation signaling. Key pharmacologic effects include inhibition of VEGFR1-3 and TIE2 to reduce angiogenesis, inhibition of PDGFR and certain FGFR isoforms to disrupt tumor stroma and vascular support, and inhibition of oncogenic kinases such as KIT, RET and RAF family members to reduce tumor cell proliferation and survival. Active metabolites, principally the N-oxide and N-desmethyl forms, are pharmacologically active and contribute to the observed antitumor effects.
Life expectancy cannot be stated as a single value because outcomes depend on the tumor type, stage, prior therapies, performance status and response to treatment. Clinical trial median overall survival examples provide context: in refractory metastatic colorectal cancer the CORRECT trial reported a median overall survival around 6.4 months for regorafenib-treated patients versus about 5.0 months for placebo, in hepatocellular carcinoma the RESORCE study after prior sorafenib reported a median overall survival around 10.6 months, and in gastrointestinal stromal tumor trials regorafenib demonstrated progression-free survival benefit. Individual prognosis varies widely and should be discussed with the treating oncologist.
Pricing for regorafenib in India varies by brand (branded Stivarga versus generic formulations), tablet strength, pack size and purchase channel, and can change over time; branded product is typically high cost and may be dispensed through hospital or specialty pharmacies, while approved generics and patient assistance programs can substantially reduce out-of-pocket expense. For an accurate and current price consult licensed oncology pharmacies, hospital procurement, a treating oncologist or official manufacturer/distributor channels.
