STX-241 / Pierre Fabre, Antares Therapeutics - LARVOL DELTA

First-In-Human Trial of PFL-241/STX-241 in Patients With Locally Advanced or Metastatic NSCLC Resistant to EGFR Tyrosine Kinase Inhibitors (IASLC-WCLC 2025) - "PFL-241/STX-241 is highly selective for EGFR mutants over wild-type, and has brain penetrance comparable to osimertinib. Part 3, will assess the efficacy of PFL-241/STX-241 at the RP2D. PFL-241 is approved for enrollment in 5 countries globally with 10 actively recruiting patients"

Clinical • Metastases • P1 data • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • EGFR

Pierre Fabre Laboratories Strengthen R&D Portfolio and Announce the Acquisition of the Worldwide Rights for PFL-721 and PFL-241 (The Manila Times) - "Pierre Fabre Laboratories are pleased to announce the acquisition from Antares Therapeutics, Inc. ('Antares'), a spin-out of Scorpion Therapeutics, Inc., of the worldwide rights for PFL-721 and PFL-241 (formerly known as STX-721 and STX-241, respectively). Under the terms of the agreement, Pierre Fabre Laboratories will expand its previous agreement with Scorpion Therapeutics to hold the global rights for both assets and will be leading the clinical development of both programs....'With this agreement with Antares, Pierre Fabre Laboratories now own the global rights for all the assets within our R&D portfolio: exarafenib, PFL-002 (formerly VERT-002), PFL-721 and PFL-241'."

M&A • Non Small Cell Lung Cancer

Pierre Fabre's fourth-generation EGFR-TKI is first approved for clinical trials in China [Google translation] (bydrug.pharmcube.com) - "The latest announcement on the CDE official website shows that the Class 1 new drug STX-241 tablets submitted by Pierre Fabre have been approved for clinical use. It is intended to treat patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) resistant to third-generation EGFR TKI treatment."

New trial • Non Small Cell Lung Cancer

STX-241 FIH: Study of FIH of STX-241 in Locally Advanced or Metastatic NSCLC Resistant to EGFR TKIs (clinicaltrials.gov) - P1/2 | N=171 | Recruiting | Sponsor: Pierre Fabre Medicament | Not yet recruiting ➔ Recruiting

Enrollment open • Metastases • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Pierre Fabre Laboratories and Scorpion Therapeutics Announce First Patient Dosed in Phase I/II Clinical Trial of PFL-241/STX-241, a Mutant-Selective Inhibitor Intended To Treat Locally Advanced or Metastatic Non-Small Cell Lung Cancer (PRNewswire) - "Pierre Fabre Laboratories...and Scorpion Therapeutics, Inc...announced that the first patient has been dosed in a Phase I/II, first-in-human dose-escalation, dose-optimization and dose-expansion trial. This clinical trial evaluates PFL-241/STX-241, a highly differentiated, orally bioavailable, highly selective tyrosine kinase inhibitor ('TKI') targeting epidermal growth factor receptor ('EGFR') Exon 19 or 21 mutations with the co-occurring C797S mutation, a known resistance mechanism to 3rd generation EGFR inhibitors."

Trial status • Non Small Cell Lung Cancer

STX-241 FIH: Study of FIH of STX-241 in Locally Advanced or Metastatic NSCLC Resistant to EGFR TKIs (clinicaltrials.gov) - P1/2 | N=171 | Not yet recruiting | Sponsor: Pierre Fabre Medicament

Metastases • New P1/2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Scorpion Therapeutics Announces $150 Million Series C Financing to Advance Leading Clinical-stage Precision Oncology Pipeline (Businesswire) - "Scorpion Therapeutics, Inc...announced the closing of a $150 million Series C financing....Scorpion plans to use the proceeds from this financing to advance its pipeline of differentiated small molecule oncology programs, in particular, to expand clinical development of its allosteric, differentiated, mutant-selective PI3Kα inhibitor, STX-478. Further, the Company will continue to advance its clinical-stage EGFR inhibitor franchise, including STX-721 and STX-241, and its discovery pipeline of next-generation precision oncology therapies."

Financing • Oncology • Solid Tumor

Scorpion Therapeutics Presents Preclinical Data for STX-241, a Fourth-Generation EGFR Inhibitor, at the AACR-NCI-EORTC Symposium 2023 (Businesswire) - "Scorpion Therapeutics, Inc...announced preclinical data for STX-241, an orally bioavailable, highly selective, central nervous system ('CNS')-penetrant and potentially best-in-class fourth generation epidermal growth factor receptor ('EGFR') tyrosine kinase inhibitor ('TKI') designed to inhibit C797S mutations with a co-occurring EGFR exon 19 deletion or exon 21 mutation ('double mutant') in non-small cell lung cancer ('NSCLC')....In these studies, STX-241 demonstrated strong biochemical inhibition of EGFR double mutant kinase activity, as well as strong C797S double mutant potency and selectivity across both proliferation and target engagement assays, exceeding clinical-stage competitor benchmarks in each of these model systems....STX-241 is currently advancing through preclinical studies, and Scorpion expects to submit an IND to the U.S. FDA in the first half of 2024."

IND • Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Identification of STX-241, a CNS-penetrant and mutant-selective EGFR inhibitor with activity on osimertinib-resistant C797x mutations. (AACR-NCI-EORTC 2023) - No abstract available

Oncology

Scorpion Therapeutics Nominates STX-241 as Potentially Best-in-Class Fourth-Generation EGFR Inhibitor Development Candidate for the Treatment of Non-Small Cell Lung Cancer (Businesswire) - "Scorpion Therapeutics, Inc...announced that it has named STX-241 as its next development candidate....In preclinical studies, STX-241 demonstrated potential best-in-class mutant vs. wild-type selectivity for the EGFR exon 19/C797S and EGFR exon 21/C797S double mutations when compared to key reference benchmarks, including approved first- and third-generation EGFR TKIs, gefitinib and osimertinib, which could translate into a wide therapeutic index. In addition, treatment with STX-241 demonstrated tumor regressions in animal models and favorable CNS penetration. Scorpion expects to present these data in the second half of 2023 and to submit an IND filing in the first half of 2024."

IND • Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology

Scorpion Therapeutics and Pierre Fabre Announce Collaboration and License Agreement to Co-Develop and Commercialize STX-721 and STX-241 for Patients with EGFR Mutant Non-Small Cell Lung Cancer (Businesswire) - "Scorpion Therapeutics, Inc...and Pierre Fabre...announced an exclusive collaboration and license agreement for the co-development of STX-721 and STX-241, two candidates in Scorpion’s franchise of highly-selective, next-generation mutant epidermal growth factor receptor ('EGFR') inhibitors....Under the agreement, Scorpion will lead clinical development of STX-721 and Pierre Fabre will lead clinical development of STX-241. Scorpion will retain commercialization rights to STX-721 and STX-241 in the United States, Canada and Japan, and Pierre Fabre will be responsible for commercialization activities in all other territories, with a focus on Europe and China."

Licensing / partnership • Lung Cancer • Non Small Cell Lung Cancer • Oncology