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...
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.
Lilly to acquire Scorpion Therapeutics' mutant-selective PI3Kα ...
2 days ago · 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 …
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 …
LBA27 First-in-human results of STX-478, a mutant-selective PI3Ka ...
STX-478 is an oral, allosteric, CNS-penetrant, mutant-selective PI3Kα inhibitor designed to improve efficacy while sparing WT toxicities. STX-478 led to robust efficacy without WT toxicities in PI3Kα mutant (PI3Kαm) tumors in vivo. Initial Phase 1 monotherapy trial results are reported.
Clinical Trials Using Mutant-selective PI3K-alpha H1047X Inhibitor STX-478
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.
Abstract P4-07-04: STX-478, a mutant-selective PI3Kα H1047X …
Mar 1, 2023 · STX-478 is an allosteric, CNS-penetrant, selective PI3Kα H1047X inhibitor, having excellent drug-like properties and exceptional kinome selectivity. STX-478 demonstrated minimal inhibition of CYP enzymes in vitro, supporting the potential for combinations with a wide range of therapeutics in breast cancer and a variety of other tumor types.
- Some results have been removed