Actively Recruiting
TSL2109 Capsules in Advanced Solid Tumor Patients: Safety, Tolerability, PK and Preliminary Efficacy
Led by Tasly Pharmaceutical Group Co., Ltd · Updated on 2026-04-07
78
Participants Needed
1
Research Sites
44 weeks
Total Duration
On this page
AI-Summary
What this Trial Is About
TSL2109 is a novel CDK4/6-DYRK2 dual-target inhibitor developed by Jiangsu Tasly Diyee Pharmaceutical Co., Ltd. for solid tumor treatment. Preclinical studies confirm its selective targeting of CDK4/6 and DYRK2, a eukaryotic CMGC family kinase. In palbociclib-resistant cell lines, TSL2109 downregulates cell cycle-related proteins and DYRK2 pathway ribosomal synthesis regulators (RRS1, CDK2), and upregulates p53, thus exerting synergistic antitumor effects and overcoming resistance to enzalutamide and palbociclib. As a small-molecule inhibitor with novel targets, structure and mechanism, TSL2109 blocks tumor cell cycle progression independently of hormonal signaling. Preclinical studies show it overcomes AR inhibitor resistance, meeting unmet needs for prostate cancer patients progressing after AR inhibitor therapy. It also reduces CDK2 activity and blocks CDK4/6 compensatory mechanisms, reversing resistance to CDK4/6 inhibitors, providing a new option for HR+/HER2- advanced breast cancer patients. Participants Dose-Escalation Phase: Advanced solid tumor patients, prioritizing metastatic castration-resistant prostate cancer (mCRPC) and HR+/HER2- advanced breast cancer. Dose-Expansion Phase: Cohort A/C: mCRPC; Cohort B/D: HR+/HER2- advanced breast cancer. Treatment Regimens C0 Cycle (3 days): Single oral dose on Day 1 morning under fasting, followed by 72-hour observation. C1 Cycle (28 days): Daily fasting oral dosing (QD) for 3 weeks, then 1-week rest. Participants may continue treatment if no DLT and potential clinical benefit. Dose escalation to a pre-established tolerable level is allowed per investigator-sponsor agreement if well-tolerated and likely beneficial. Treatment continues until disease progression, intolerable toxicity or new antitumor therapy. The Dose-Expansion Phase uses the same regimen as C1. Missed Dose: Make-up within 8 hours; skip if delayed over 8 hours. Notes: Once MTD is determined, participants dosed above MTD will be adjusted to MTD. All doses are administered orally under fasting conditions.
CONDITIONS
Official Title
TSL2109 Capsules in Advanced Solid Tumor Patients: Safety, Tolerability, PK and Preliminary Efficacy
Who Can Participate
Eligibility Criteria
You may qualify if you...
- Age 18 years or older
- Histologically or cytologically confirmed advanced solid tumors with failure of or no available standard therapy, or unsuitable for standard therapy, not amenable to curative surgery or radiotherapy
- Priority given to metastatic castration-resistant prostate cancer and HR+/HER2- advanced breast cancer
- At least one evaluable or measurable tumor lesion per RECIST Version 1.1
- Life expectancy of 3 months or more
- ECOG performance status of 0 to 1
- For mCRPC: receiving androgen deprivation therapy or history of bilateral orchiectomy, serum total testosterone ≤1.7 nmol/L, and documented disease progression
- For HR+/HER2- breast cancer: confirmed HR-positive, HER2-negative status, locally advanced or recurrent/metastatic breast cancer in females
- Prior exposure to CDK4/6 inhibitors for breast cancer patients
You will not qualify if you...
- Symptomatic central nervous system or leptomeningeal metastases or uncontrolled CNS disease
- Diagnosis of another invasive cancer within past 2 years except certain treated non-melanoma skin cancers and in situ carcinomas
- Significant gastrointestinal dysfunction affecting drug absorption
- Tumor invasion of major blood vessels with bleeding risk
- Interstitial lung disease, pneumonitis, or pulmonary fibrosis deemed unsuitable
- History of deep vein thromboembolism
AI-Screening
AI-Powered Screening
Complete this quick 3-step screening to check your eligibility
Trial Site Locations
Total: 1 location
1
Shanghai Gaobo Cancer Hospital (China Pharmaceutical University)
Shanghai, Shanghai Municipality, China, 200003
Actively Recruiting
Research Team
R
Rui Liu
CONTACT
How is the study designed?
Study Type
INTERVENTIONAL
Masking
NONE
Allocation
NA
Model
SINGLE_GROUP
Primary Purpose
TREATMENT
Number of Arms
1
Not the Right Trial for You?
Explore thousands of other clinical trials that might be a better match.
Sign up to get personalized trial recommendations delivered to your inbox.
Already have an account? Log in here