TY-0540 / TYK Medicines - LARVOL DELTA

Safety and preliminary efficacy of a novel CDK2/4 inhibitor TYK-00540 in patients with advanced solid tumors: Results from a phase I dose-escalation study (ESMO 2025) - "These findings support the ongoing phase II study evaluating TYK-00540 in combination with fulvestrant to further explore its potential in addressing this unmet clinical need. Legal entity responsible for the study TYK Medicines."

Clinical • Metastases • P1 data • Breast Cancer • Oncology • Solid Tumor • HER-2

CLINICAL STUDY OF TYK-00540 (HKEXnews) - "Clinical positive data for CDK inhibitors announced at ESMO Congress 2025....As of July 15, 2025, a total of 24 patients were enrolled in the monotherapy dose-escalation stage, including 16 patients who had previously received CDK4/6i treatment....Among the 13 patients with HR+/HER2- BC available for evaluation, 2 patients achieved confirmed partial response (PR) and 5 achieved stable disease (SD), representing an objective response rate (ORR) of 15.4% (2/13) and a disease control rate (DCR) of 53.8% (7/13)."

P1 data • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

Study of TYK-00540 Combined With Enzalutamide in Patients With Metastatic Castration-resistant Prostate Cancer（mCRPC） (clinicaltrials.gov) - P1/2 | N=48 | Not yet recruiting | Sponsor: TYK Medicines, Inc

New P1/2 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

PHASE I CLINICAL TRIAL RESULTS OF TY-302, TY-2699a AND TY-0540 ACCEPTED FOR POSTER PRESENTATION AT THE 2025 EUROPEAN SOCIETY FOR MEDICAL ONCOLOGY (ESMO) CONGRESS (HKEXnews) - "The board of directors (the 'Board') of the Company is pleased to announce that the Phase I clinical trial results for three internally-developed clinical products of the Company, namely TY-302, TY-2699a, and TY-0540, have been officially accepted for poster presentation at the 2025 European Society for Medical Oncology (ESMO) Congress. Relevant detailed data from the trials will be presented during the conference....Data accepted for presentation comes from a Phase I multicenter combination therapy clinical trial (NCT04433494)...a Phase I multicenter monotherapy dose-escalation clinical trial (NCT05866692)...[and]...a Phase I multicenter open-label clinical trial (NCT06246071)."

P1 data • Solid Tumor

Study of TYK-00540 Tablets in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=180 | Recruiting | Sponsor: TYK Medicines, Inc

New P1/2 trial • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

TYK Medicine’s CDK2 Inhibitor Receive Clinical Approval from CDE for Combination Therapy (TYK Medicines Press Release) - "TYK Medicine announced that its self-developed next-generation oral, highly potent small molecule CDK2 inhibitor, TYK-00540, has received formal approval from the Center for Drug Evaluation (CDE) of the National Medical Products Administration to proceed with Phase II clinical trial for combination therapy. The company is going to initiate the trial recently to accelerate the clinical development of TYK-00540....The Phase II clinical trial approval will further advance the development of TYK-00540 for CDK4/6 inhibitor-resistant breast cancer and prostate cancer indications, positioning it as a promising candidate in TYK Medicine’s oncology pipeline to solve the unmet medical needs."

New P2 trial • Breast Cancer • Prostate Cancer

ASOTIAPWST: A Study of TYK-00540 in Adult Patients With Solid Tumors (clinicaltrials.gov) - P1 | N=156 | Recruiting | Sponsor: TYK Medicines, Inc

New P1 trial • Oncology • Solid Tumor

TY-0540, a highly potent CDK2/4/6 inhibitor, attenuates acquired resistance against CDK4/6 inhibition (AACR 2023) - "To test the effectiveness of the clinical candidate compound on CDK4/6i resistance models, two Palbociclib resistant cell populations (T47D-R, HCC1428-R) were in-house generated via gradient exposure of the cells to Palbociclib. #Meihua Li and Chengshan Niu contributed equally to this work. *Jun Li, Meihua Li and Chengshan Niu are the correspondent authors."

Preclinical • Breast Cancer • HER2 Breast Cancer • Oncology • Solid Tumor • CCNE1 • CDK1 • CDK7 • CDK9 • E2F1 • ER • FOXM1 • HER-2 • MYC