Antineoplastic API Infigratinib (CAS 872511-34-7) Pharmaceutical Grade White Fine Powder

Infigratinib More Info

Infigratinib is an orally bioavailable, small molecule, ATP-competitive inhibitor of fibroblast growth factor receptors, with the CAS Registry Number 872511-34-7. Its molecular structure is specifically designed to bind with high selectivity and potency to the ATP-binding domain of FGFR 1, 2, and 3, particularly in their dysregulated or mutated states commonly found in certain cancers. This targeted design aims to block the downstream signaling of the FGFR pathway, which drives tumor cell proliferation, survival, and angiogenesis. The compound is a key representative of a newer generation of precision oncology drugs.

The primary mechanism of action is the selective inhibition of FGFR tyrosine kinase activity. By binding to the intracellular kinase domain, infigratinib prevents autophosphorylation and activation of the receptor, thereby blocking the downstream RAS-MAPK and PI3K-AKT signaling cascades. This inhibition is especially potent in tumors harboring FGFR gene alterations, such as fusions, amplifications, or activating mutations, which create a state of oncogenic addiction to this pathway. The therapeutic effect is to halt the growth and promote the death of these dependent cancer cells.

The main clinical application of infigratinib is in the treatment of advanced or metastatic cholangiocarcinoma in adults who have progressed after prior therapy and whose tumors harbor an FGFR2 fusion or rearrangement, as detected by an approved test. It represents a paradigm of biomarker-driven therapy for this aggressive biliary tract cancer. It is also under investigation in other solid tumors with relevant FGFR alterations, such as urothelial carcinoma and certain types of gastric cancer.

This medication is administered orally in capsule form, typically taken once daily on an empty stomach for 21 consecutive days followed by 7 days off, constituting a 28-day treatment cycle. This schedule helps manage potential side effects. Its pharmacokinetics involve extensive metabolism, primarily by cytochrome P450 3A4, necessitating dose adjustments when used concomitantly with strong CYP3A4 inhibitors or inducers. Regular monitoring of phosphate levels is required due to its unique toxicity profile.

The safety profile of infigratinib is characterized by both on-target and off-target effects. The most frequent and notable adverse events are related to on-target FGFR inhibition and include hyperphosphatemia (often managed with dietary modifications or phosphate binders), nail toxicity, stomatitis, dry eye, and fatigue. Serious risks include retinal pigment epithelial detachment, which requires regular ophthalmologic exams, and the potential for embryo-fetal toxicity. Common laboratory abnormalities include increased creatinine and alkaline phosphatase. Its use requires careful patient selection based on molecular testing and proactive management of its distinct toxicities.