STX-721 / Pierre Fabre, Antares Therapeutics - LARVOL DELTA

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

Trial in progress: First-in-human study of PFL-721/STX-721 in participants with locally advanced or metastatic non-small cell lung cancer harboring EGFR exon 20 insertion mutations. (ASCO 2025) - P1/2 | "Amivantamab, a bispecific anti-EGFR/c-MET-receptor antibody, is approved for the treatment of NSCLC with EGFR ex20ins mutations. Finally, Part 3 will further test the anticancer efficacy of PFL-721/STX-721 is administered at the RP2D. PFL-721/STX-721-101 is actively enrolling at 18 sites in 7 countries globally."

EGFR exon 20 • Metastases • P1 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR • HER-2 • MET

STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models. (PubMed, Clin Cancer Res) - "In carefully benchmarked biochemical, biophysical, and cellular assays, STX-721 demonstrated superior ex20ins-mutant selectivity relative to other tested benchmark clinical phase compounds and achieved ex20ins-mutant-selective tumor regression in vivo. These data highlight that STX-721 shows a high level of mutant EGFR selectivity across human preclinical cancer models and may provide an improved clinical efficacy versus adverse event profile relative to existing drugs."

Journal • Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR • HER-2

First-In-Human Study of STX-721 in Participants With Locally Advanced or Metastatic Non-Small Cell Lung Cancer Harboring EGFR Exon 20 Insertion Mutations (clinicaltrials.gov) - P1/2 | N=185 | Recruiting | Sponsor: Antares Therapeutics, Inc | N=120 ➔ 185

Enrollment change • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Discovery of STX-721, a Covalent, Potent, and Highly Mutant-Selective EGFR/HER2 Exon20 Insertion Inhibitor for the Treatment of Non-Small Cell Lung Cancer. (PubMed, J Med Chem) - "STX-721 (53) is a potent, irreversible inhibitor of the majority of EGFR/HER2 ex20ins mutants and demonstrates excellent mutant vs wild-type selectivity both in vitro and in vivo. STX-721 is currently in phase 1/2 clinical trials for EGFR/HER2 ex20ins-driven NSCLC."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR • HER-2

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

First-In-Human Study of STX-721 in Participants With Locally Advanced or Metastatic Non-Small Cell Lung Cancer Harboring EGFR Exon 20 Insertion Mutations (clinicaltrials.gov) - P1/2 | N=120 | Recruiting | Sponsor: Scorpion Therapeutics, Inc. | Not yet recruiting ➔ Recruiting | Trial primary completion date: Jul 2026 ➔ Jun 2027

EGFR exon 20 • Enrollment open • HER2 exon 20 • Metastases • Trial primary completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Scorpion Therapeutics and Pierre Fabre Laboratories Announce First Patient Dosed in Phase 1/2 Clinical Trial of STX-721, a Mutant-Selective EGFR Exon 20 Inhibitor for the Treatment of Locally Advanced or Metastatic Non-Small Cell Lung Cancer (PRNewswire) - "Scorpion Therapeutics...and Pierre Fabre Laboratories today announced that the first patient has been dosed in a Phase 1/2 first-in-human dose escalation and expansion clinical trial evaluating STX-721, Scorpion's highly differentiated, orally bioavailable, irreversible highly selective tyrosine kinase inhibitor ('TKI') targeting epidermal growth factor receptor ('EGFR') and ERBB2 (HER2) Exon 20 insertion ('ex20ins') mutations, well-known, clinically validated oncogenic drivers in non-small cell lung cancer ('NSCLC'). The Phase 1/2 clinical trial will evaluate STX-721 as a monotherapy in participants with locally advanced or metastatic NSCLC harboring EGFR ex20ins mutations."

EGFR exon 20 • Trial status • Non Small Cell Lung Cancer

First-In-Human Study of STX-721 in Participants With Locally Advanced or Metastatic Non-Small Cell Lung Cancer Harboring EGFR Exon 20 Insertion Mutations (clinicaltrials.gov) - P1/2 | N=120 | Not yet recruiting | Sponsor: Scorpion Therapeutics, Inc.

EGFR exon 20 • HER2 exon 20 • Metastases • New P1/2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Discovery of STX-721, a potent and Mutant-Selective EGFR exon 20 inhibitor with a potential best-in-class profile (ACS-Fall 2023) - "Approved and investigational therapies for NSCLC patients with EGFR exon 20 insertion mutations have only demonstrated moderate clinical efficacy (28-52% ORR), compared to Osimertinib's significant 70-80% ORR activity in the more common EGFR mutant tumors. Here we disclose for the first time the structure and optimization efforts that led to the discovery of STX-721, a highly-differentiated EGFR/HER2 inhibitor that provides superior exon 20 insertion mutation vs. wild type selectivity relative to approved and clinical benchmarks across in vitro and in vivo model biological systems, including in vivo isogenic/matched human cancer cell line models. STX-721 has the potential to provide a best-in-class profile to improve outcomes in patients harboring cancers with EGFR/HER2 exon 20 mutations and has completed investigational new drug (IND)-enabling studies with a favorable risk/benefit profile supporting clinical development."

EGFR exon 20 • Gastrointestinal Disorder • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

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

Identification of STX-721, an EGFR exon 20 mutant inhibitor with superior selectivity and a potential best-in-class profile (AACR-NCI-EORTC 2022) - "STX-721 demonstrates EGFR exon 20 mutant selectivity approaching the selectivity of Osimertinib in EGFR T790M mutants, warranting further exploration of this potential best-in-class exon 20 inhibitor in the clinic. Ba/F3: proliferation selectivity vs. EGFR WT Human cells: proliferation selectivity (vs."

EGFR exon 20 • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

STX-721 shows efficacy and selectivity in EGFR exon 20 mutant models (Bioworld) - "Researchers from Scorpion Therapeutics Inc. presented preclinical data for the novel EGFR exon 20 mutant inhibitor STX-721, being developed for the treatment of non-small-cell lung cancer (NSCLC)."

EGFR exon 20 • Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Scorpion Therapeutics Presents Preclinical Proof-of-Concept Data for STX-721, a Next-Generation Exon 20 Mutant EGFR Inhibitor, at the EORTC-NCI-AACR Symposium 2022 (Businesswire) - "Investigational new drug ('IND') application submission expected in 2023...In these studies, STX-721 demonstrated strong EGFR exon 20 mutant potency and selectivity in isogenic Ba/F3 models and human cancer cell lines, as well as signaling and biochemical assays. Importantly, the selectivity of STX-721 for EGFR exon 20 was observed to well exceed that of clinical-stage competitor benchmarks in each of these model systems, while also approaching the selectivity of osimertinib against EGFR L858R and exon 19 deletion mutations. In addition, STX-721 demonstrated strong in vivo anti-tumor activity across a variety of EGFR and HER2 exon 20 mutant cell line-derived xenograft ('CDX') and patient-derived xenograft ('PDX') models. STX-721 also demonstrated a clear exon 20 genotype-selective in vivo efficacy window in isogenic cancer CDX models, which was not observed with clinical-stage competitor benchmarks."

IND • Preclinical • Oncology • Solid Tumor

Scorpion Therapeutics to Present Preclinical Proof-of-Concept Data for Highly Selective, Next-Generation Exon 20 Mutant EGFR Inhibitor at 34th EORTC-NCI-AACR Symposium (Businesswire) - "Scorpion Therapeutics, Inc...announced that it will present preclinical proof-of-concept data for STX-721 in a poster session at the European Organisation for Research and Treatment of Cancer, the National Cancer Institute, and the American Association for Cancer Research ('EORTC-NCI-AACR') Symposium 2022 in Barcelona, Spain, taking place October 26 – 28, 2022....STX-721 is progressing through preclinical studies and Scorpion expects to submit an IND application to the U.S. Food and Drug Administration in 2023."

EGFR exon 20 • IND • Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Scorpion Therapeutics Nominates STX-721 as EGFR-EXON-20 Development Candidate with a Best-in-Class Profile (Businesswire) - "Scorpion Therapeutics, Inc...announced that it has selected STX-721 as a development candidate from its STX-EGFR-EXON20 program. Scorpion Therapeutics expects to present these preclinical data at a medical meeting in the second half of 2022 and to submit an IND for STX-721 in 2023."

EGFR exon 20 • IND • Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Scorpion Therapeutics Reveals Highly-selective Lead Programs Targeting Mutant PI3Kα and EGFR Exon 20, Two Established Cancer Drivers with Broad Therapeutic Applicability (Businesswire) - "Scorpion Therapeutics, Inc...revealed its two lead programs, both targeting well-known, clinically validated, mutated oncogenes. The first program, STX-H1047-PI3Kα, targets the H1047X-mutant form of phosphoinositide 3-kinase alpha ('PI3Kα'), a cancer driver associated with a wide variety of solid tumors. The second program, STX-EGFR-EXON20, selectively targets exon 20 insertion mutations in epidermal growth factor receptor ('EGFR'), which drives non-small cell lung cancer ('NSCLC')...Scorpion expects to submit an IND for STX-H1047-PIK3α in 2023....Scorpion expects to submit an IND for STX-EGFR-EXON20 in 2023."

Clinical • EGFR exon 20 • IND • Lung Cancer • Non Small Cell Lung Cancer • Oncology