Kolupin (tunlametinib) / KeChow Pharma - LARVOL DELTA

A phase III, randomized, open-label study of tunlametinib plus vemurafenib versus investigator's choice of therapy in patients with previously treated BRAFV600E-mutant metastatic colorectal cancer. (ASCO 2026) - P1, P3 | "This is the first phase III randomized controlled trial to demonstrate that a BRAF/MEK inhibitor combination (tunlametinib plus vemurafenib) significantly improves PFS and ORR compared with conventional chemotherapy-based regimens in previously treated BRAF V600E–mutant mCRC, with a manageable safety profile and the added benefit of a convenient all-oral regimen."

Clinical • Late-breaking abstract • Metastases • P3 data • Colorectal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Efficacy and safety of tunlametinib in patients with advanced NRAS-mutant melanoma: A multicenter, open-label, single-arm, phase 2 study. (ASCO 2023) - P2 | "Tunlametinib was well tolerated and demonstrated encouraging treatment response rate in pts with advanced NRAS-mutant melanoma. These results indicate that tunlametinib could be a promising treatment option for NRAS-mutant melanoma, even for those immunotherapy failed pts. Clinical trial information: NCT05217303."

Clinical • IO biomarker • Metastases • P2 data • Melanoma • Mucosal Melanoma • Oncology • Solid Tumor • NRAS

Tunlametinib in Combination With Pucotenlimab and Hydroxychloroquine in NRAS Mutant Melanoma (clinicaltrials.gov) - P2 | N=37 | Recruiting | Sponsor: Sun Yat-sen University

IO biomarker • New P2 trial • Melanoma • Oncology • Solid Tumor • NRAS

Efficacy and Safety of Tunlametinib Combination Therapy in the Treatment of Second-line and Above Metastatic Colorectal Cancer (clinicaltrials.gov) - P2 | N=91 | Not yet recruiting | Sponsor: Sun Yat-sen University

New P2 trial • Colorectal Cancer • Oncology • Solid Tumor • BRAF • MSI

DTP-HER2: A Study of Disitamab Vedotin, Tunlametinib, and PD-1 Antibody for Advanced Gastric Cancer (clinicaltrials.gov) - P2 | N=76 | Not yet recruiting | Sponsor: Sun Yat-sen University

New P2 trial • Gastric Adenocarcinoma • Gastric Cancer • Oncology • Solid Tumor • HER-2

SUCCESSFUL TREATMENT OF SECONDARY HISTIOCYTIC SARCOMA AFTER B-ALL TRANSPLANTATION WITH TARGETED THERAPY COMBINED WITH RADIOTHERAPY: A CASE REPORT (EBMT 2026) - "The decitabine and a single reinfusion of the donor's cryopreserved peripheral blood stem cells were administered.In June 2022, the patient presented fever without responding to anti-infective treatment...Consideration of Disease progression, trametinib was discontinued due to presumed drug resistance.On 21st June 2024, the patient started on oral MEK1/2 inhibitor tunlametinib at a dose of 12 mg twice daily which induced severe Skin and soft tissue infection after 4 weeks, necessitating a dose reduction to 6 mg twice daily without interruption of therapy...Tunlametinib was combined with one dose of ipilimumab... This patient presents with a rare secondary HS following B-ALL transplant. There is no standardized or consistently effective treatments. Patients who are gene test positive, targeted therapies can be considered."

Case report • Clinical • Acute Lymphocytic Leukemia • B Acute Lymphoblastic Leukemia • Bone Marrow Transplantation • Hematological Malignancies • Infectious Disease • Leukemia • Sarcoma • Solid Tumor • Transplantation • ARAF • BRCA2 • FANCC • NF1 • PTPN11 • SF3A1 • SH2B3

Tunlametinib Combination Therapy in KRAS-Mutated Unresectable Locally Advanced or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov) - P2 | N=55 | Not yet recruiting | Sponsor: Sun Yat-sen University

New P2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • KRAS

Efficacy of Tunlametinib in Combination With Anti-EGFR Monoclonal Antibody in Patients With RAS-Mutated Advanced Gastrointestinal Malignancies (clinicaltrials.gov) - P2 | N=90 | Not yet recruiting | Sponsor: Chinese PLA General Hospital

New P2 trial • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Pancreatic Cancer • Solid Tumor

RWS of Tunlametinib in NRAS-Mutant Advanced Melanoma (clinicaltrials.gov) - P4 | N=110 | Recruiting | Sponsor: Fudan University

New P4 trial • Real-world evidence • Melanoma • Oncology • Solid Tumor • NRAS

Efficacy and Safety of Tunlametinib in Adults with Inoperable Neurofibromatosis Type 1-Associated Plexiform Neurofibromas: Phase IIa Trial and Biomarker Research. (PubMed, Clin Cancer Res) - "Tunlametinib demonstrated promising efficacy and an acceptable safety profile in adults with PN, broadly aligning with prior PN trial including selumetinib and mirdametinib."

Biomarker • Journal • P2a data • Genetic Disorders • Neurofibromatosis • Solid Tumor

Melanoma: Pathogenesis and Targeted Therapy. (PubMed, MedComm (2020)) - "In recent years, MEK inhibitors like binimetinib and tunlametinib have displayed the efficacy for NRASmut melanoma, with tunlametinib being the first and only approved MEK inhibitor for advanced NRASmut melanoma. Subsequently, we explored current and potential treatment approaches for melanoma, primarily encompassing BRAF inhibitors, MEK inhibitors, and immunotherapy, with a particular focus on their clinical relevance of development. Finally, the challenges in the treatment of melanoma, particularly in immunotherapy and targeted therapy, are summarized and discussed."

IO biomarker • Journal • Review • Tumor mutational burden • Melanoma • Oncology • Skin Cancer • Solid Tumor • NF1 • NRAS • TMB

Tunlametinib + AG + Cetuximab β as First-Line Therapy for Advanced Pancreatic Cancer (clinicaltrials.gov) - P4 | N=28 | Not yet recruiting | Sponsor: Tianjin Medical University Cancer Institute and Hospital

New P4 trial • Oncology • Pancreatic Cancer • Solid Tumor

Multimodal treatment with thiotepa, bevacizumab, teniposide, and tunlametinib in a patient with neurofibromatosis type 1-associated oligodendroglioma: a rare case report. (PubMed, Anticancer Drugs) - "As of June 2025, the patient has achieved a CR with a progression-free survival of 9 months before experiencing disease recurrence. This rare case of NF1-associated oligodendroglioma was managed with thiotepa, bevacizumab, teniposide, and tunlametinib, highlighting the potential of MEK inhibition in NF1-related gliomas."

Journal • Brain Cancer • Genetic Disorders • Glioma • Neurofibromatosis • Oligodendroglioma • Oncology • Solid Tumor • NF1

Phase II Trial of Tunlametinib in Patients With NRAS Mutant Non-melanoma Refractory Solid Tumors (clinicaltrials.gov) - P2 | N=15 | Recruiting | Sponsor: Tianjin Medical University Second Hospital

New P2 trial • Non-melanoma Skin Cancer • Oncology • Solid Tumor

A prospective, single-arm, open-label exploratory clinical study evaluating the efficacy and safety of the combination therapy of toramatinib, vemurafenib and cetuximab in the first-line treatment of unresectable or advanced BRAF V600E mutant colorectal cancer (ChiCTR) - P4 | N=5 | Not yet recruiting | Sponsor: Ruijin Hospital, Shanghai Jiao Tong University School of Medicine; Ruijin Hospital, Shanghai Jiao Tong University School of Medicine

New P4 trial • Colorectal Cancer • Oncology • Solid Tumor • BRAF

IIT-085-TC-002: Phase II Trial of Tunlametinib in NRAS-Mutant Advanced Thyroid Cancer (clinicaltrials.gov) - P2 | N=40 | Recruiting | Sponsor: Fudan University | Not yet recruiting ➔ Recruiting

Enrollment open • Oncology • Solid Tumor • Thyroid Gland Carcinoma

Characterization of 12 Unknown Photodegradation Impurities of Tunlametinib Capsules Using Liquid Chromatography Coupled With ion Trap/Time-Of-Flight Mass Spectrometry. (PubMed, Rapid Commun Mass Spectrom) - "Structural elucidation of 12 previously uncharacterized photodegradation impurities was achieved through HPLC/IT-TOF MS. These findings establish a scientific foundation for refining quality specifications of tunlametinib."

IO biomarker • Journal • Melanoma • Neuroblastoma • Oncology • Solid Tumor • NRAS

A Study Evaluating the Efficacy and Safety of Torametinib (HL085) in Combination with Fruquintinib and Hydroxychloroquine (HCQ) in Patients with RAS/BRAFV600E Mutation-Positive Refractory Advanced Colorectal Cancer (ChiCTR) - P2 | N=38 | Not yet recruiting | Sponsor: Peking Union Medical College Hospital; Peking Union Medical College Hospital

New P2 trial • Colon Adenocarcinoma • Colon Cancer • Colorectal Cancer • Oncology • Solid Tumor • BRAF • KRAS • NRAS

Novel Therapies for Neurofibromatosis Type 1-Associated Inoperable Plexiform Neurofibromas: A Systematic Literature Review (ISPOR 2025) - "These reported on a total of 21 unique studies on 11 emerging therapies: 6 MEK inhibitors (selumetinib, mirdametinib, trametinib, binimetinib, FCN-159, tunlametinib) and 5 targeted anti-cancer agents (cabozantinib, tipifarnib, sorafenib, sirolimus, everolimus)... The promising results of MEK inhibitors in therapeutic trials for NF1 demonstrate that targeting the MAPK/ERK pathway is an attractive therapeutic avenue for unresectable PNs. Because selumetinib is only approved for children, future reimbursement will require advanced studies establishing MEK inhibitor efficacy in adults."

Review • Brain Cancer • Genetic Disorders • Neurofibromatosis • Oncology • Solid Tumor • NF1

Targeting the MAPK Pathway for NRAS Mutant Melanoma: From Mechanism to Clinic. (PubMed, Br J Dermatol) - "In recent years, significant clinical advancements have been achieved by targeting the NRAS-MAPK pathway, with novel therapies such as the MEK inhibitor tunlametinib and the combination therapy of the pan-RAF inhibitor naporafenib with trametinib leading the way. In this review, we will systematically summarize the recent advances in the direct targeting of mutant NRAS proteins and their downstream RAF and MEK proteins, as well as targeting the MAPK pathway in combination with other therapeutic targets, including the immunotherapy, to treat NRAS mutant melanoma. Additionally, we will further discuss the current issues and emerging countermeasures related to targeted therapy for NRAS mutant melanoma."

IO biomarker • Journal • Melanoma • Oncology • Solid Tumor • NRAS

An Exploratory Clinical Study Evaluating the Efficacy and Safety of Tunlametinib Combined With Fruquintinib in the Third-line Treatment of Advanced Colorectal Cancer Patients With RAS Mutations. (clinicaltrials.gov) - P=N/A | N=34 | Not yet recruiting | Sponsor: Liu Huang

New trial • Colorectal Cancer • Oncology • Solid Tumor

IIT-085-TC-002: A Prospective, Single-Arm, Open-Label, Single-Center Phase II Exploratory Clinical Study to Evaluate the Efficacy and Safety of Tunlametinib in Subjects With NRAS-Mutant Locally Advanced or Metastatic Thyroid Cancer (clinicaltrials.gov) - P2 | N=40 | Not yet recruiting | Sponsor: Fudan University

New P2 trial • Endocrine Cancer • Oncology • Solid Tumor • Thyroid Gland Anaplastic Carcinoma • Thyroid Gland Carcinoma

Efficacy and Safety of Tunlametinib Plus Vemurafenib in Patients With BRAF V600E-mutant Metastatic Colorectal Cancer (clinicaltrials.gov) - P3 | N=165 | Recruiting | Sponsor: Shanghai Kechow Pharma, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Colorectal Cancer • Oncology • Solid Tumor • BRAF

Tunlametinib: First Approval. (PubMed, Drugs) - "In March 2024, tunlametinib was granted conditional approval in China (based on surrogate endpoints) for use in patients with NRAS-mutated advanced melanoma who have failed anti-PD-1/PD-L1 treatment. This article summarizes the milestones in the development of tunlametinib leading to this first approval for the treatment of solid tumours with RAS and RAF mutations."

IO biomarker • Journal • Review • Colorectal Cancer • Gastrointestinal Cancer • Genetic Disorders • Lung Cancer • Melanoma • Neurofibromatosis • Non Small Cell Lung Cancer • Oncology • Solid Tumor • MAP2K1 • NF1 • NRAS

Comparing Tunlametinib Capsules and Combination Chemotherapy in Advanced NRAS-mutant Melanoma (clinicaltrials.gov) - P3 | N=165 | Recruiting | Sponsor: Shanghai Kechow Pharma, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • IO biomarker • Metastases • Melanoma • Oncology • Solid Tumor • NRAS