THE-349 / Concentra Biosci - LARVOL DELTA

Preclinical characterization of THE-349, a mutant-selective, CNS-active, fourth-generation EGFR inhibitor to overcome T790M- and C797S-mediated resistance in NSCLC. (AACR-NCI-EORTC 2023) - No abstract available

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

Theseus Pharmaceuticals to Discontinue Enrollment in Phase 1/2 Study and Terminate Development of THE-630 in Patients with GIST (PRNewswire) - "Advance THE-349 into clinical studies: THE-349 is a potentially best-in-class fourth-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) for the treatment of EGFR mutant non-small cell lung cancer....IND-enabling toxicology studies have been completed, and Theseus remains on track to submit an Investigational New Drug Application (IND) for THE-349 in the fourth quarter of 2023, and commence its clinical program as soon as possible thereafter, subject to clearance of the IND by the U.S. Food and Drug Administration."

IND • New trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Theseus Pharmaceuticals Announces Business Highlights and Reports First Quarter 2023 Financial Results (PRNewswire) - "Research and development expenses were $12.4 million for the first quarter of 2023, as compared to $6.5 million for the same period in 2022. This increase was primarily due to a $2.7 million increase in expense for preclinical studies and drug manufacturing to support THE-349 IND enabling studies, a $1.4 million increase in development expense related to discovery programs, as well as a $1.5 million increase in employee-related costs driven by an increase in headcount."

Commercial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thoracic Cancer

Theseus Pharmaceuticals Highlights Key Anticipated 2023 Milestones and Announces BCR-ABL as Target for Third Development Program (PRNewswire) - "Progressing Phase 1/2 clinical trial of THE-630 in advanced GIST; preliminary dose-escalation data anticipated in Q2 2023 with additional data expected in Q4 2023; IND submission for 4G EGFR inhibitor THE-349 expected in Q4 2023; Introducing BCR-ABL as target for third program, in development for CML and Ph+ ALL; development candidate nomination expected by early 2024."

IND • P1/2 data • Pipeline update • B Acute Lymphoblastic Leukemia • Chronic Myeloid Leukemia • Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Hematological Malignancies • Leukemia • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Theseus Pharmaceuticals Announces Business Highlights and Reports Fourth Quarter and Full Year 2022 Financial Results (Yahoo News) - "THE-349 is a fourth-generation (4G) epidermal growth factor receptor (EGFR) TKI development candidate with activity against single-, double-, and triple-mutant EGFR variants, including T790M and C797X, found in EGFR-mutant non-small cell lung cancer (NSCLC) that has developed resistance to first- or later-line osimertinib....Theseus expects to submit an Investigational New Drug Application (IND) for THE-349 to the U.S. Food and Drug Administration (FDA) in the fourth quarter of 2023 and to initiate the clinical program as soon as possible thereafter, subject to clearance of the IND by the FDA."

IND • New trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

"THE-349, a Fourth-Generation EGFR Inhibitor will be coming for rescue, hopefully by next year end." (@drakhilkapoor1)

Theseus Pharmaceuticals Presents Preclinical Data Characterizing THE-349, its Fourth-Generation EGFR Inhibitor in Development for NSCLC, at the 34th EORTC-NCI-AACR Symposium (PRNewswire) - "IND submission to US FDA anticipated in H2 2023....In vitro: THE-349 potently inhibits both major classes of EGFR activating mutations – exon 19 deletions (D) and L858R (L) – alone, or in combination with one or both major resistance mutations – T790M (T) and C797X; including C797S (C) and two other variants that drive resistance to osimertinib...In vivo: THE-349 induces robust anti-tumor activity, with deep and sustained tumor regressions observed at well-tolerated doses, in mouse models expressing single-, double- and triple-mutant EGFR; Strong regressions (>80% tumor regressions) against osimertinib-resistant C797S double (LC) and triple mutants (LTC and DTC), directly addressing EGFR-mediated resistance after first-line and second-line osimertinib, respectively; Deep and/or complete tumor regression in an osimertinib-resistant, patient-derived (PDX) NSCLC model harboring heterogeneous EGFR mutant variants (D and DTC)."

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

Theseus Pharmaceuticals Nominates THE-349, a Fourth-Generation EGFR Inhibitor Development Candidate in Non-Small Cell Lung Cancer (PRNewswire) - "IND submission anticipated in H2 2023....Theseus Pharmaceuticals, Inc...announced that it has nominated THE-349 as the development candidate for its epidermal growth factor receptor (EGFR) inhibitor program in non-small cell lung cancer (NSCLC)....In preclinical models, THE-349 potently inhibits single-, double-, and triple-mutant EGFR variants with these mutations that are observed in a post-first- or later-line osimertinib setting....Preclinical characterization of THE-349 as a fourth-generation EGFR, central nervous system- (CNS) active, and mutant-selective inhibitor with potent activity against single-, double-, and triple-mutant EGFR variants, including T790M and C797X, will be shared in a poster presentation at the 34th EORTC-NCI-AACR (ENA) Symposium taking place in Barcelona on October 26-28, 2022."

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

Discovery of potent and selective next-generation EGFR inhibitors with activity against single, double, and triple mutant EGFR variants including T790M and C797S (AACR 2022) - "Introduction: EGFR activating mutations are observed in 10-50% of NSCLC patients and the common mutations (L858R [L] and exon 19 deletions [D]) are initially sensitive to first-, second-, and third-generation EGFR inhibitors (eg erlotinib [1G], afatinib [2G], and osimertinib [3G], respectively). We have identified a series of next-generation EGFR inhibitors with potent in vitro and in vivo activity against single, double, and triple mutant EGFR variants including T790M and C797S."

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

Theseus Pharmaceuticals Announces Preclinical Data Characterizing Next-Generation Epidermal Growth Factor Receptor (EGFR) Inhibitors at the 2022 American Association for Cancer Research (AACR) Annual Meeting (PRNewswire) - "Theseus Pharmaceuticals...announced preclinical data characterizing next-generation pan-variant EGFR inhibitors that will be detailed in a live poster presentation at the American Association for Cancer Research (AACR) 2022 Annual Meeting, being held April 8-13, 2022 in New Orleans, Louisiana. The poster highlights advanced lead compounds for use in non-small cell lung cancer (NSCLC) that have been observed to potently inhibit the kinase activity, both in vitro and in vivo, of all major single-, double-, and triple-mutant EGFR variants, including T790M and C797S, with selectivity over wild-type EGFR and the ability to penetrate the central nervous system (CNS)....Nomination of development candidate expected in Q3 2022; IND expected in 2023."

IND • Pipeline update • Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thoracic Cancer

Theseus Pharmaceuticals Announces Business Highlights and Reports Fourth Quarter and Full Year 2021 Financial Results (PRNewswire) - "Theseus expects to nominate an EGFR candidate designed to inhibit the full range of single-, double-, and triple-mutant EGFR variants found in the tumors of patients with EGFR-mutant NSCLC that have developed resistance to osimertinib, including the C797S mutation. Preclinical data is expected to be presented at the American Association for Cancer Research (AACR) Annual Meeting in April and at a scientific conference in the second half of 2022. IND submission is expected in 2023."

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

Theseus Pharmaceuticals to Present Preclinical Data Characterizing Next-Generation Epidermal Growth Factor Receptor (EGFR) Inhibitors at the 2022 American Association for Cancer Research (AACR) Annual Meeting (PRNewswire) - "Theseus Pharmaceuticals, Inc...announced that the Company will present a poster highlighting the characterization of potent and selective next-generation EGFR inhibitors at the American Association for Cancer Research (AACR) 2022 Annual Meeting, being held April 8-13, 2022 in New Orleans, Louisiana."

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