Pyrazoles are organic compounds of the general formula C3H3N2H. It is a five-membered heterocycle consisting of three carbon atoms and two adjacent nitrogen atoms. As an H-bond-donating heterocycle, pyrazole has been used as a more lipophilic and metabolically more stable bioisomer of phenol. Pyrazoles have attracted more and more attention due to their broad spectrum of action and strong efficacy.
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IDRx announces $120 million series B financing to advance potential best-in-class new treatment for gastrointestinal stromal tumor (GIST). IDRX-42 is a potent, oral, highly selective KIT inhibitor targeting all major categories of activating and resistance mutations in patients with KIT-mutant GIST (including variants in exons 9, 11, 13 and 17). IDRX-42 was granted Orphan Drug designation by the FDA for the treatment of GIST. IDRX-42 is currently being evaluated in StrateGIST 1, a first-in-human Phase 1/1b study.
In preclinical studies, IDRX-42 demonstrated superior antitumor activity compared to imatinib, the current first-line of therapy, in GIST human xenograft models expressing mutations in KIT exons 9 and 11. In xenograft models expressing secondary resistance mutations in KIT exon 13 or 17, IDRX-42 treatment resulted in potent and dose-dependent antitumor activity superior to the second-line standard of care agent, sunitinib.
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