Overview

The primary objective of Phase I of this study is to evaluate the safety and tolerability, and to determine the maximum tolerated dose (MTD) or recommended phase 2 dose (RP2D) of CTS3497 in patients with metastatic or locally advanced methylthioadenosine phosphorylase (MTAP)-deficient solid tumors and lymphomas.

The primary objective of Phase II of this study is to evaluate the efficacy of CTS3497 in patients with metastatic or locally advanced MTAP-deficient solid tumors and lymphomas.

Eligibility

Inclusion Criteria:

• ≥ 18 years of age at the signing of ICF.
• Patients with histologically or cytologically confirmed locally advanced or metastatic solid tumors who cannot be treated surgically and have failed standard of care (SoC). Or patients with refractory/relapsed lymphomas.
• MTAP deficiency is confirmed by IHC or NGS.
• At least one evaluable tumor lesion at screening for patients in escalation part, and at least one measurable tumor lesion for patients in expansion part.
• ECOG performance status of 0 to 1.
• Adequate hematopoietic function, cardiac function, liver function, renal function, and coagulation function per local laboratory.

Exclusion Criteria:

• Female patients in pregnancy or lactation.
• Patients with dysphagia; or a condition that seriously affects gastrointestinal absorption.
• Allergic or intolerant to the active ingredients or excipients of the investigational product.
• Anti-tumor therapy within 28 days of study day 1.
• Prior treatment with an methionine adenosyltransferase 2α (MAT2A) inhibitor or a protein arginine methyltransferase 5 (PRMT5) inhibitor.
• Central nervous system (CNS) metastasis at screening.
• Live vaccine therapy within 4 weeks before study drug administration.
• Use of therapeutic anti-coagulation for treatment of active thromboembolic events.
• Use of prescription medications that are known strong inducers or inhibitors of cytochrome P450 3A4 (CYP3A4) within 14 days or 5 half-lives (whichever is longer) before study day 1.
• Unresolved toxicity from prior anti-cancer therapy.
• Active infection of HIV, HBV or HCV.
• Patients who are judged by the investigator to have a history of other serious systemic diseases, or not suitable for participating in the trial for any other reason.