Inavolisib

DelveInsight's 'Breast Cancer Pipeline Insight 2024' highlights a robust pipeline with 100+ companies developing 120+ drugs, driven by rising incidence, tech advancements, and increased awareness. Key companies and drugs include Ambrx, CSPC ZhongQi, Merus, and ARX788, DP303c, SHR-A1811, among others. FDA fast-track designations and breakthrough therapy designations for drugs like 9MW2821 and inavolisib underscore significant progress.

Roche agreed to pay $850 million to acquire two experimental breast cancer drugs from Regor Therapeutics. These 'next-generation' CDK inhibitors, RGT-419B and another in early trials, aim to improve upon current CDK treatments by addressing resistance and reducing side effects. Roche plans to start a Phase 2 trial for RGT-419B in 2024, with Regor managing ongoing Phase 1 trials and Roche handling further development and commercialization.

STX-478 is an oral, CNS-penetrant, allosteric inhibitor of mutant PI3Kα, targeting a cryptic pocket near the ATP-binding site, avoiding off-target effects on WT PI3Kα and other kinases.

CRAFT interim analysis shows inavolisib (GDC-0077) promising in disease control for rare tumors, with 36% disease control rate in PIK3CA-mutated tumors. Presented at ESMO 2024, ongoing CRAFT trial aims to confirm efficacy and safety across various disease states.

Inavolisib (GDC-0077) showed a favorable safety profile and disease control rates of 60% at week 8 and 32% at week 16 in patients with refractory, PIK3CA-mutated solid tumors, according to the phase 2 CRAFT trial. The median progression-free survival was 3.52 months, and the 12-month overall survival rate was 51%. The most common PIK3CA mutations were E545K, E542K, and H1047R/L, with 7 patients achieving disease control at week 16. Adverse effects included hyperglycemia, diarrhea, fatigue, and constipation, mostly at grade 1 or 2.

FDA grants Priority Review to Roche's inavolisib for advanced HR+/HER2- breast cancer with PIK3CA mutation, based on Phase III INAVO120 results showing significant progression-free survival benefits.