-1%
Regocent is classified as a targeted cancer therapy for various malignancies, including metastatic colorectal cancer, GIST, and hepatocellular carcinoma.
Regocent (Regorafenib) is a small molecule that works by inhibiting multiple kinases associated with cellular functions and abnormal processes like cancer, tumor blood vessel formation (angiogenesis), metastasis, and immune response to tumors. Regorafenib and its active metabolites (M-2 and M-5) block the activities of various receptors like RET, VEGFR1-3, KIT, PDGFR, FGFR1-2, and others, which are essential for the development and spread of tumors. Preclinical studies showed that Regorafenib inhibited tumor growth in several models, including those for colorectal cancer, GIST, and HCC.
Absorption, Distribution, Metabolism, and Elimination:
- Absorption: After a single dose of 160 mg, Regocent achieves a peak plasma concentration (Cmax) of 2.5 µg/mL at 4 hours and an area under the curve (AUC) of 70.4 µgh/mL. At steady state, Cmax increases to 3.9 µg/mL, and AUC reaches 58.3 µgh/mL.
- Distribution: Regorafenib is highly protein-bound (99.5%) and undergoes enterohepatic circulation.
- Metabolism: Regorafenib is metabolized primarily by CYP3A4 and UGT1A9, with M-2 and M-5 being the major metabolites.
- Excretion: Around 71% of the administered dose is excreted in feces, while 19% is excreted through urine.