TY-2699a / TYK Medicines - LARVOL DELTA

A phase I dose-escalation study of TY-2699a, a non-covalent inhibitor of CDK7, in patients with advanced solid tumors (ESMO 2025) - P1 | "Conclusions Continuous BID dosing of TY-2699a reached high dose levels with a manageable safety profile and early antitumor activity. Further study in intermittent regimens and combinations is warranted."

Clinical • Metastases • P1 data • Breast Cancer • Colorectal Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Lung Cancer • Oncology • Oral Cancer • Ovarian Cancer • Small Cell Lung Cancer • Solid Tumor • Tongue Carcinoma • Triple Negative Breast Cancer • CDK7 • ER • HER-2

CLINICAL STUDY OF TY-2699A (HKEXnews) - "Clinical positive data for CDK inhibitors announced at ESMO Congress 2025....This Phase I clinical study, employing a BOIN design, enrolled 20 patients with advanced solid tumors across five dose-escalation cohorts....3 patients achieved SD, including one with TNBC in the 5mg cohort and two with HR+/HER2- mBC in the 20mg and 30mg cohorts respectively, all of whom are still receiving treatment in their respective cohorts."

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

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

A potent CDK7 inhibitor TY-2699a suppresses palbociclib-resistant breast cancer and has the potential for combination with chemotherapy or immunotherapy in solid tumors (AACR 2025) - "The efficacy of CT-7001 monotherapy at a dose of 100 mg/kg was comparable to that of TY-2699a at a dose of 1 mg/kg, which only mildly inhibited tumor growth. Our efficacy data of TY-2669a provides a solid rationale for further evaluation of TY-2699a +/- fulvestrant in clinical HR+Her2- CDK4/6-resistant breast cancer patients. In addition, targeted inhibition of CDK7 not only enhanced the efficacy of paclitaxel or gemcitabine in pancreatic cancer cells, but also enhanced the in vivo efficacy of nab-paclitaxel, gemcitabine, and nab-paclitaxel in combination with gemcitabine in mouse pancreatic cancer tumor models...In the single-agent dose escalation stage, TY-2699a showed better clinical safety than SY-5609 did... TY-2699a was more than 80-, 66- and 86-fold more active than palbociclib in palbociclib-resistant stable cell lines of MCF7, T47D and HCC1428 cells, respectively. Consistent with the in vitro results, a 40 mg/kg dose of palbociclib almost completely failed to..."

IO biomarker • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Nasopharyngeal Carcinoma • Oncology • Pancreatic Cancer • Solid Tumor • CDK6 • ER • HER-2

TYK Medicine’s CDK7 Inhibitor TY-2699a Receives CDE Clinical Approval for Combination Therapy (TYK Medicines Press Release) - "TYK Medicine announced that its independently developed next-generation oral, highly potent, and highly selective small-molecule CDK7 inhibitor, TY-2699a, has received official approval from the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA) to conduct clinical trials for the treatment of advanced solid tumors in combination with different regimens."

New trial • Oncology • Solid Tumor

INTERIM RESULTS ANNOUNCEMENT FOR THE SIX MONTHS ENDED JUNE 30, 2024 (HKEXnews) - "We are currently conducting a Phase I clinical trial of TY-2699a monotherapy or combination therapy in locally advanced or metastatic solid tumors (especially in SCLC and triple-negative breast cancer ('TNBC') in China. We expect to commence Phase Ib clinical trial in the first quarter of 2025...TY-4028 is a potent, irreversible, oral exon 20 insertion-TKI, targeting locally advanced or metastatic NSCLC with EGFR exon 20 or HER2 exon 20 insertions....We plan to initiate a Phase I trial of TY-4028 in NSCLC with exon 20 insertion in China in December 2024."

New P1 trial • Trial status • Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor • Triple Negative Breast Cancer • Exon 20

A Study of TY-2699a in Patients With Locally Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - P1 | N=156 | Recruiting | Sponsor: TYK Medicines, Inc | Not yet recruiting ➔ Recruiting

Enrollment open • Metastases • Breast Cancer • HER2 Breast Cancer • Hormone Receptor Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor • Triple Negative Breast Cancer • BRCA • ER • HER-2 • KRAS • PD-L1

A Study of TY-2699a in Patients With Locally Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - P1 | N=156 | Not yet recruiting | Sponsor: TYK Medicines, Inc

Metastases • New P1 trial • Breast Cancer • HER2 Breast Cancer • Hormone Receptor Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor • Triple Negative Breast Cancer • BRCA • ER • HER-2 • KRAS • PD-L1

TY-2699a is a highly potent CDK7 inhibitor to abolish dysfunctional tumor cell cycle for clinical development (AACR 2023) - P1 | "Currently, trilaciclib, palbociclib, ribociclib, and abemaciclib that bear dual specificities against CDK4 and CDK6 have been approved for clinical usage, and more CDK4/6 targeted agents are actively under clinical evaluations, among which, TY-302, a novel CDK4/6 inhibitor being developed by TYK Medicines, is under Phase II trial (NCT04433494)...Several CDK7 targeted agents, such as SY-5609 and Samuraciclib (CT7001), are under development...# Shengli Dong and Apeng Liang contributed equally to this work. * Jun Li, Shengli Dong and Apeng Liang are the correspondent authors."

Clinical • Tumor cell • Acute Myelogenous Leukemia • Breast Cancer • Gastrointestinal Cancer • Lung Cancer • Neuroendocrine Tumor • Oncology • Ovarian Cancer • Pancreatic Cancer • Small Cell Lung Cancer • Solid Tumor • Triple Negative Breast Cancer • CCNA2 • CCND1 • CCNE1 • CDK1 • CDK2 • CDK7