THE-630 / Concentra Biosci - LARVOL DELTA

A Study of THE-630 in Patients With Advanced Gastrointestinal Stromal Tumors (GIST) (clinicaltrials.gov) - P1/2 | N=32 | Terminated | Sponsor: Theseus Pharmaceuticals | Active, not recruiting ➔ Terminated; The Sponsor terminated the study due to early dose-limiting toxicities.

Metastases • Stroma • Trial termination • Gastroenterology • Gastrointestinal Cancer • Gastrointestinal Disorder • Gastrointestinal Stromal Tumor • Oncology • Sarcoma

A Study of THE-630 in Patients With Advanced Gastrointestinal Stromal Tumors (GIST) (clinicaltrials.gov) - P1/2 | N=32 | Active, not recruiting | Sponsor: Theseus Pharmaceuticals | Recruiting ➔ Active, not recruiting | N=160 ➔ 32 | Trial completion date: Jun 2026 ➔ Feb 2024 | Trial primary completion date: Jun 2025 ➔ Feb 2024

Enrollment change • Enrollment closed • Metastases • Stroma • Trial completion date • Trial primary completion date • Gastroenterology • Gastrointestinal Cancer • Gastrointestinal Disorder • Gastrointestinal Stromal Tumor • Oncology • Sarcoma

Theseus (THRX) Falls 72% on Decision to Discontinue GIST Study (Nasdaq) - "Theseus Pharmaceuticals, Inc. THRX announced its decision to discontinue enrollment in its ongoing early-mid-stage study of THE-630 in patients with gastrointestinal stromal tumors (GIST). The company also terminated the development of THE-630 in GIST. The decision to discontinue the development of the candidate was taken after serious adverse events were observed in patients, following treatment with the candidate. The stock of the company plunged 72% on Friday in response to the dismal news."

Discontinued • Stock price • Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Oncology • Solid Tumor

Theseus Pharmaceuticals to Discontinue Enrollment in Phase 1/2 Study and Terminate Development of THE-630 in Patients with GIST (PRNewswire) - "Theseus Pharmaceuticals...announced that it is discontinuing enrollment in the ongoing phase 1/2 study and terminating development of THE-630 in patients with gastrointestinal stromal tumors (GIST)....As of July 10, 2023, 32 patients have been treated with THE-630 across 7 dose levels (3 mg to 27 mg). Six patients developed grade 1 to 3 HFSR (3 patients in the 27 mg cohort, 2 patients in the 18 mg cohort, and 1 patient originally in the 9 mg cohort after intra-patient dose escalation to 18 mg)....The Company does not believe that THE-630 has a differentiated profile at doses below 27 mg, which would provide exposure well below the target level of 100 nanomolar average concentration. As a result, the Company has made the decision to terminate the development of THE-630 in GIST. Patients currently enrolled in the trial will continue to receive THE-630 until a treatment discontinuation criterion is met."

Discontinued • Enrollment status • Gastrointestinal Stromal Tumor • Oncology • Solid Tumor

Initial results from the phase (ph) 1 portion of a ph 1/2 study of THE-630 in patients (pts) with advanced gastrointestinal stromal tumor (GIST). (ASCO 2023) - P1/2 | "First-line imatinib provides initial clinical benefit in advanced disease, but prognosis is poor for pts whose tumors progress, despite 3 other approved tyrosine kinase inhibitors (TKIs). THE-630 had an acceptable initial safety profile, and escalation continues, as target exposure for pan-variant KIT activity is not yet reached. Reduction in KIT-mutant allele fractions in ctDNA and initial evidence of disease control were observed. Clinical trial information: NCT05160168."

Clinical • Metastases • Stroma • Anemia • Cardiovascular • Dyslipidemia • Dyspepsia • Fatigue • Gastrointestinal Cancer • Gastrointestinal Disorder • Gastrointestinal Stromal Tumor • Hematological Disorders • Hypertension • Myocardial Infarction • Oncology • Pulmonary Disease • Sarcoma • Xerostomia

Theseus Pharmaceuticals Reports Initial Dose Escalation Data from Ongoing Phase 1/2 Trial of THE-630 in Patients with Advanced GIST (PRNewswire) - P1/2 | N=160 | NCT05160168 | Sponsor: Theseus Pharmaceuticals | "Theseus Pharmaceuticals, Inc...announced initial dose escalation data from the ongoing phase 1/2 trial of THE-630 in patients with advanced gastrointestinal stromal tumors (GIST)....Following the data cutoff, both Cohort 7 patients subsequently cleared the dose-limiting toxicity (DLT) observation period without experiencing a DLT....Disease stabilization was observed more frequently at higher doses, with 8 out of 9 evaluable patients treated in Cohorts 4-6 (9 to 18 mg) achieving stable disease as best response, a disease control rate of 89%. A patient with 5 prior lines of therapy and KIT exon 11 and exon 17 (N822K) mutations detected in ctDNA at baseline had prolonged stable disease, receiving THE-630 for 36 weeks (enrolled in Cohort 2 [4 mg] with subsequent escalation to 6 mg and then 9 mg), with strong ctDNA reductions of both mutations observed."

P1/2 data • Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Oncology • Solid Tumor

Theseus Pharmaceuticals Initial Dose Escalation Results from Ongoing Phase 1/2 Trial of THE-630 Accepted for Online Publication at 2023 ASCO Annual Meeting (PRNewswire) - "Theseus Pharmaceuticals...announced that initial dose escalation data from the ongoing phase 1/2 study of THE-630 in advanced gastrointestinal stromal tumors (GIST) were accepted for online publication at the 2023 American Society of Clinical Oncology (ASCO) Annual Meeting....The data to be presented from the ongoing dose escalation study are expected to include preliminary safety, pharmacokinetic (PK), and clinical activity data through cohort 6, as well as an analysis of circulating tumor DNA (ctDNA) data through cohort 5."

P1/2 data • Gastrointestinal Stromal Tumor • Oncology • Sarcoma • Soft Tissue Sarcoma • Solid Tumor

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 (PRNewswire) - "Enrollment is ongoing for the phase 1 portion of the phase 1/2 dose-escalation and expansion clinical trial evaluating THE-630 in patients with advanced GIST, with all seven phase 1 sites open in the U.S. and accruing. Theseus is treating patients in cohort 6 of dose escalation as of March 9, 2022. Theseus plans to present preliminary safety, pharmacokinetic (PK), and initial clinical activity data through cohort 6, as well as an analysis of circulating tumor DNA (ctDNA) data up to cohort 5, at a scientific conference in the second quarter of 2023. Theseus plans to present follow-up data at a scientific conference in the fourth quarter of 2023, which is expected to include data from additional dose escalation cohorts, including cohorts 7 and 8..."

P1/2 data • PK/PD data • Trial status • Gastrointestinal Stromal Tumor • Oncology • Sarcoma • Soft Tissue Sarcoma • Solid Tumor

Theseus Pharmaceuticals Announces Business and Pipeline Highlights and Reports Third Quarter 2022 Financial Results (PRNewswire) - "Recent Pipeline Highlights and Upcoming Expected Milestones:...A Phase 1/2 dose-escalation and expansion clinical trial evaluating THE-630 in patients with advanced GIST is ongoing. Phase 1 site activation was completed in the third quarter of 2022 and the study continues to enroll patients in the dose-escalation portion of the trial. Initial safety and pharmacokinetic data, as well as initial analysis of circulating tumor DNA, from the dose-escalation portion of the clinical trial are expected to be presented at a scientific conference in the second quarter of 2023. Additional data from the Phase 1 portion of the clinical trial is expected to be presented in the fourth quarter of 2023."

P1 data • Trial status • Gastrointestinal Stromal Tumor • Oncology • Sarcoma • Solid Tumor

Theseus Pharmaceuticals Receives U.S. FDA Orphan Drug Designation for THE-630 for the Treatment of Advanced Gastrointestinal Stromal Tumors (GIST) (PRNewswire) - "Theseus Pharmaceuticals...announced that the U.S. Food and Drug Administration (FDA) has granted orphan drug designation (ODD) to the company's lead candidate THE-630, a small-molecule oral pan-variant KIT inhibitor, for the treatment of patients with advanced gastrointestinal stromal tumors (GIST)."

Orphan drug • Gastrointestinal Stromal Tumor • Oncology • Sarcoma • Solid Tumor

Theseus Pharmaceuticals Announces First Patient Treated with THE-630 in Phase 1/2 Study in Patients with Advanced Gastrointestinal Stromal Tumors (GIST) (PRNewswire) - "Theseus Pharmaceuticals...announced that the first patient has been treated in the Phase 1 portion of Theseus' ongoing Phase 1/2 study to evaluate lead candidate, THE-630, in patients with advanced gastrointestinal stromal tumors (GIST)....Initial data from the Phase 1 portion of the clinical trial is expected to be presented at a scientific meeting in the first half of 2023."

P1 data • Trial status • Gastrointestinal Stromal Tumor • Oncology • Solid Tumor

A Study of THE-630 in Patients With Advanced Gastrointestinal Stromal Tumors (GIST) (clinicaltrials.gov) - P1/2; N=160; Recruiting; Sponsor: Theseus Pharmaceuticals; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open • Gastroenterology • Gastrointestinal Cancer • Gastrointestinal Disorder • Gastrointestinal Stromal Tumor • Oncology • Sarcoma

A Study of THE-630 in Patients With Advanced Gastrointestinal Stromal Tumors (GIST) (clinicaltrials.gov) - P1/2; N=160; Not yet recruiting; Sponsor: Theseus Pharmaceuticals

Clinical • New P1/2 trial • Gastroenterology • Gastrointestinal Cancer • Gastrointestinal Disorder • Gastrointestinal Stromal Tumor • Oncology • Sarcoma

Theseus Pharmaceuticals Announces FDA Clearance of Investigational New Drug Application for THE-630, a Pan-Variant KIT Inhibitor in Development for the Treatment of Gastrointestinal Stromal Tumors (GIST) (PRNewswire) - "Theseus Pharmaceuticals...announced U.S. Food and Drug Administration (FDA) clearance of an investigational new drug (IND) application to evaluate THE-630...in patients with gastrointestinal stromal tumors (GIST). THE-630 is a pan-variant inhibitor of the receptor tyrosine kinase KIT designed for patients with advanced GIST whose cancer has developed resistance to earlier lines of therapy....Theseus plans to initiate a Phase 1/2 dose escalation and expansion clinical trial of THE-630 in patients with previously treated advanced GIST between late fourth quarter 2021 and mid-first quarter 2022."

IND • New P1/2 trial • Gastrointestinal Stromal Tumor • Oncology • Sarcoma

[VIRTUAL] Preclinical characterization of THE-630, a next-generation inhibitor for KIT-mutant gastrointestinal stromal tumors (GIST) (AACR 2021) - "Prognosis is poor for patients whose tumors progress following first-line (1L) imatinib treatment, despite availability of 3 approved drugs (sunitinib [2L], regorafenib [3L], ripretinib [4L]). We have identified a next-generation pan-KIT inhibitor that has potent activity against all major classes of activating and resistance mutations observed in KIT-mutant GIST patients. A phase 1 clinical trial of THE-630 is planned to begin in 2021."

Preclinical • Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Oncology • Sarcoma • Solid Tumor

Theseus Pharmaceuticals Debuts with $100M Series B Raise to Develop Pan-Variant Kinase Inhibitors (PRNewswire) - “Theseus Pharmaceuticals…announcing the close of a $100 million Series B financing led by Foresite Capital. Theseus also announced data from a poster presentation at the American Association for Cancer Research (AACR) 2021 Annual Meeting, which demonstrated that the Company's lead product candidate, THE-630, has potent activity against all major classes of activating and resistance mutations observed in patients with KIT-mutant gastrointestinal stromal tumors (GIST)…The Company expects to file an IND before the end of the year. Theseus' pipeline also includes a selective EGFR inhibitor to overcome C797S-mediated resistance to first- or later-line osimertinib treatment for patients with non-small cell lung cancer, and a third kinase target candidate for an undisclosed indication.”

Financing • IND • Preclinical • Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Sarcoma • Solid Tumor • Thoracic Cancer