STX-478 demonstrated in vivo efficacy and safety in preclinical models superior to clinically-relevant doses of alpelisib, a non-mutant selective PI3Kα inhibitor Efficacious in PI3Kα E542K
Scorpion Therapeutics Provides Clinical Program Updates for Its …
Scorpion has shown in Phase 1 monotherapy data that STX-478, an oral, once-daily, mutant-selective, allosteric PI3Kα inhibitor, demonstrated robust PI3Kα pathway inhibition as a monotherapy, with anti-tumor activity observed in multiple cancer types, including a 23% overall response rate (ORR) in HR+/HER2- breast cancer (BC) and a 44% ORR in gyn...
STX-478 - Drug Hunter
STX-478 is a wild-type-sparing, oral, CNS-penetrant, novel allosteric inhibitor of mutant PI3Kα (phosphatidylinositol-3 kinase α) targeting a cryptic pocket near the ATP-binding site. PI3Kα plays a central role in many cancers, and has been recently highlighted in coverage of 2021 Molecule of the Year nominee and PI3Kα degrader inavolisib.
Scorpion Therapeutics Announces First Patient Dosed in Phase 1/2 ...
STX-478 is designed to improve outcomes in patients harboring prevalent PI3Kα mutations in their tumors and has shown activity in both kinase and helical domain mutated tumors in preclinical models.
First-in-Human Study of STX-478, a Mutant-Selective PI3Ka …
Study STX-478-101 is a multipart, open-label, phase 1/2 study evaluating the safety, tolerability, pharmacokinetics (PK), and preliminary antitumor activity of STX-478 in participants with advanced solid tumors with P13Ka mutations.
STX-478: Profile • STX-478 binds to a novel, cryptic allosteric site present in both mutant and WT PI3Kαisoforms8 • STX-478 has activity against the most common PI3Kαkinase-domain mutation H1047R (inhibitory concentration [IC 50] = 9.4 nmol/L), with 14-fold selectivity over WT PI3Kα(IC 50= 131 nmol/L)8
STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares ...
Nov 1, 2023 · Here we describe STX-478, an allosteric PI3Kα inhibitor that selectively targets prevalent PI3Kα helical- and kinase-domain mutant tumors. STX-478 demonstrated robust efficacy in human tumor xenografts without causing the …
Lilly to acquire Scorpion Therapeutics' mutant-selective PI3Kα ...
Jan 13, 2025 · The acquisition will expand Lilly's oncology pipeline with STX-478, the differentiated and potentially best-in-class, mutant-selective PI3Kα inhibitor currently in a Phase 1/2 clinical trial. STX-478 could potentially address 30-40% of people with hormone-positive breast cancer, building on Lilly's advancements against this disease
STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares ...
Nov 1, 2023 · Here we describe STX-478, an allosteric PI3Kα inhibitor that selectively targets prevalent PI3Kα helical- and kinase-domain mutant tumors. STX-478 demonstrated robust efficacy in human tumor xenografts without causing the …
RCSB PDB - 8TDU: STX-478, a Mutant-Selective, Allosteric …
Jul 5, 2023 · Here we describe STX-478, an allosteric PI3Kα inhibitor that selectively targets prevalent PI3Kα helical- and kinase-domain mutant tumors. STX-478 demonstrated robust efficacy in human tumor xenografts without causing the …
- Some results have been removed