TVB-3567 / Sagimet Biosci, Ascletis - LARVOL DELTA

Anticipated Upcoming Milestones (GlobeNewswire) - "Following the completion of the Phase 1 PK clinical trial of the combination of denifanstat and resmetirom, Sagimet plans to advance the development of the combination into a Phase 2 proof-of-concept trial for patients living with MASH with F4 fibrosis, expected to initiate in the second half of 2026, subject to consultation with regulatory authorities. Upon completion of the Phase 1 clinical trial of TVB-3567, and subject to consultation with regulatory authorities, Sagimet anticipates starting a Phase 2 clinical trial with TVB-3567 in moderate to severe acne patients in 2026."

New P2 trial • Acne Vulgaris • Metabolic Dysfunction-Associated Steatohepatitis

Phase 1 Study to Evaluate the Safety, Tolerability, PK, and PD of TVB-3567 in Healthy Participants With or Without Acne (clinicaltrials.gov) - P1 | N=128 | Recruiting | Sponsor: Sagimet Biosciences Inc. | Trial completion date: Jan 2026 ➔ Jun 2026 | Trial primary completion date: Dec 2025 ➔ May 2026

Trial completion date • Trial primary completion date • Acne Vulgaris

Asciminib (ASC) in Combination with Imatinib (IMA), Nilotinib (NIL), or Dasatinib (DAS) May be a Potential Treatment (Tx) Option in Patients (Pts) with Philadelphia Chromosome–Positive Chronic Myeloid Leukemia in Chronic Phase or Accelerated Phase (Ph+ CML-CP/AP): Final Results from the Asciminib Phase 1 Study (ASH 2023) - P1 | "INTRODUCTION: ATP-competitive tyrosine kinase inhibitors (TKIs) have extended the life expectancy of pts with CML. ASC in combination with ATP-competitive TKIs, while associated with a higher AE burden vs ASC monotherapy, demonstrated rapid efficacy in the enrolled pt population. The MTD for ASC + IMA was reached at ASC 60 mg QD + IMA 400 mg QD (Table); the MTD for ASC + NIL or DAS was not reached. ASC 40 or 60 mg QD + IMA 400 mg QD, ASC 40 mg BID + NIL 300 mg BID, and ASC 80 mg QD + DAS 100 mg QD were recommended doses for expansion."

Clinical • Combination therapy • P1 data • Chronic Myeloid Leukemia • Fatigue • Hematological Malignancies • Leukemia • Oncology

Asciminib (ASC) Add-on to Imatinib (IMA) Demonstrates Sustained High Rates of Ongoing Therapy and Deep Molecular Responses (DMRs) with Prolonged Follow-up in the ASC4MORE Study (ASH 2023) - P2 | "Here, we report results of ASC add-on to IMA vs continued IMA vs switch to nilotinib (NIL) and of pts who crossed over from continued IMA to ASC add-on after 96 wks of Tx in pts not achieving DMR with ≥1 y of IMA as their first TKI (cutoff: 6 Mar 2023)...The top reasons for discontinuation were pt decision (9.5% with ASC 40 mg add-on), adverse events (AEs; 14.3% and 33.3%, with ASC 60 mg add-on and NIL, respectively), and physician decision (66.7% with IMA, all of whom crossed over to ASC 60 mg add-on)... Among pts not achieving DMR after ≥1 y on IMA, more pts achieved MR4.5 with ASC add-on to IMA than with continuing IMA or switching to NIL at wk 96. Pts crossing over from IMA to ASC 60 mg add-on were still able to achieve DMRs. ASC add-on to IMA was well-tolerated, with no new or worsening safety findings compared with those known for ASC alone."

Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology

Efficacy and Safety Results from ASC4MORE, a Randomized Study of Asciminib (ASC) Add-on to Imatinib (IMA), Continued IMA, or Switch to Nilotinib (NIL) in Patients (Pts) with Chronic-Phase Chronic Myeloid Leukemia (CML-CP) Not Achieving Deep Molecular Responses (DMRs) with ≥1 Year of IMA (ASH 2022) - P2, P3 | "In the phase 3 ASCEMBL study, ASC led to superior major molecular response vs bosutinib (BOS) at wk 24 and 96...Top reasons for discontinuation were pt decision in the ASC 40-mg add-on arm (9.5%), AEs in the ASC 60-mg add-on and NIL arms (14.3% and 23.8%, respectively), and physician decision in the IMA arm (57.1%) (pts who crossed over to the ASC 60-mg add-on arm were considered discontinued for IMA arm)... More pts achieved DMR at wk 48 with ASC add-on to IMA vs continued IMA or switch to NIL in pts not achieving DMR with IMA alone for ≥1 y. In this population of pts tolerating IMA for ≥1 y, ASC add-on was generally well tolerated. While not powered to identify the best arm for achievement of DMR in this setting, the high rate of DMR in the ASC add-on arms is promising. Further studies are needed to assess if ASC alone can provide equivalent efficacy and better tolerability vs add-on to IMA."

Clinical • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology

Sagimet anticipates starting a Phase 2 clinical trial in moderate to severe acne patients in 2026 following its ongoing Phase 1 clinical trial of TVB-3567 for development of an acne indication. (GlobeNewswire)

New P2 trial • Acne Vulgaris

Sagimet Biosciences to Host Virtual KOL Event, 'A New Mechanism of Action in Treating Acne: Update on Positive Phase 3 Denifanstat Trial for the Treatment of Moderate to Severe Acne' on June 16, 2025 (GlobeNewswire) - "The event will feature key opinion leader (KOL) Neal Bhatia, MD (Director of Clinical Dermatology at Therapeutics Clinical Research in San Diego), who will join company management to review positive efficacy and tolerability results from a Phase 3 clinical trial evaluating denifanstat for the treatment of moderate to severe acne vulgaris in China conducted by Sagimet’s license partner Ascletis....In the Phase 3 study, denifanstat met all primary and secondary endpoints versus placebo and was generally well tolerated. The robust Phase 3 results underline the potential of FASN inhibition as a novel mechanism of action to address acne, a condition that impacts more than 50 million people in the U.S. annually. Management will also discuss the Company’s recently initiated Phase 1 first in-human study with its second oral FASN inhibitor drug candidate, TVB-3567, which is planned to be developed for acne in the U.S."

P3 data • Trial status • Acne Vulgaris

Phase 1 Study to Evaluate the Safety, Tolerability, PK, and PD of TVB-3567 in Healthy Participants With or Without Acne (clinicaltrials.gov) - P1 | N=128 | Recruiting | Sponsor: Sagimet Biosciences Inc.

New P1 trial • Acne Vulgaris

Sagimet Biosciences Reports First Quarter 2025 Financial Results and Provides Corporate Updates (GlobeNewswire) - "Phase 1 clinical trial to evaluate the PK and tolerability of a combination of denifanstat and resmetirom, planned to initiate in the second half of 2025, with an anticipated data readout in the first half of 2026....Ascletis BioScience Co. Ltd. (Ascletis) announced completion of enrollment of 480 patients in its Phase 3 clinical trial of denifanstat for acne in China, and that it expects to announce topline results in the second quarter of 2025. First-in-human Phase 1 clinical trial of TVB-3567 in acne expected to initiate in the second half of 2025, following the IND clearance in March 2025."

New P1 trial • P1 data • P3 data: top line • Acne Vulgaris • Metabolic Dysfunction-Associated Steatohepatitis

Sagimet Biosciences Announces Clearance of IND for FASN Inhibitor TVB-3567, to be Developed for the Treatment of Acne (GlobeNewswire) - "Sagimet Biosciences Inc...announced the clearance of its Investigational New Drug (IND) application for TVB-3567, the Company’s second fatty acid synthase (FASN) inhibitor. TVB-3567 is a potent and selective small molecule FASN inhibitor, planned to enter clinical development for the treatment of acne. The IND with the U.S. Food and Drug Administration’s Division of Dermatology and Dentistry allows the Company to initiate a first-in-human Phase 1 clinical trial of TVB-3567, planned in 2025."

IND • New P1 trial • Acne Vulgaris

Efficacy of ASC60, an oral fatty acid synthase inhibitor, in two tumor mouse models (AACR 2022) - "Previous in vitro testing showed that inhibition of palmitate synthesis by ASC60 was 137-fold lower in mouse than in human (IC50: 2.05 µM in mouse vs 0.015 µM in human). However, results of the present studies showed that ASC60 could suppress tumor growth and/or expand lifespan in the two tumor mouse models either alone or in combination with mPD-1 antibody. ASC60 will possibly demonstrate better efficacies in human."

Preclinical • Breast Cancer • Colon Cancer • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • FASN

Ascletis Announces China IND Approval of Its Second FASN Inhibitor ASC60 for Treatment of Advanced Solid Tumors (PRNewswire) - "Ascletis Pharma Inc...announces that the Investigational New Drug (IND) application of its second fatty acid synthase (FASN) inhibitor ASC60 for treatment of advanced solid tumors has been approved by China National Medical Products Administration. ASC60 IND approval further strengthens Ascletis' oncology pipeline."

Non-US regulatory • Oncology • Solid Tumor

Ascletis Announces the Latest Results of the Preclinical Studies of Two Novel Anti-Cancer Drug Candidates, ASC61 and ASC60, to be presented at AACR Annual Meeting 2022 (PRNewswire) - "Ascletis Pharma Inc...announces that the latest preclinical research results of the company's two novel anti-cancer drug candidates, ASC61, an oral PD-L1 inhibitor and ASC60, an oral fatty acid synthase (FASN) inhibitor have been selected for presentations at the American Association for Cancer Research (AACR) Annual Meeting 2022 (the '2022 AACR Annual Meeting'), and the abstracts have already been published on AACR's official website."

Preclinical • Oncology • Solid Tumor

Ascletis Announces IND Filing of Its Second FASN Inhibitor ASC60 for Advanced Solid Tumors Accepted by China NMPA (PRNewswire) - "Ascletis Pharma Inc...announces that following the consultation with China National Medical Products Administration (NMPA), the Investigational New Drug (IND) application of its second fatty acid synthase (FASN) inhibitor ASC60 for advanced solid tumors has been accepted by China NMPA. ASC60 further strengthens Ascletis' oncology pipeline."

New trial • Oncology • Solid Tumor