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    1m
    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
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    NF1 (Neurofibromin 1)
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    Avastin (bevacizumab) • Kolupin (tunlametinib) • Vumon (teniposide) • thiotepa
    3ms
    Phase II Trial of Tunlametinib in Patients With NRAS Mutant Non-melanoma Refractory Solid Tumors (clinicaltrials.gov)
    P2, N=15, Recruiting, Tianjin Medical University Second Hospital
    New P2 trial
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    MSK-IMPACT
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    Kolupin (tunlametinib)
    4ms
    IIT-085-TC-002: Phase II Trial of Tunlametinib in NRAS-Mutant Advanced Thyroid Cancer (clinicaltrials.gov)
    P2, N=40, Recruiting, Fudan University | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Kolupin (tunlametinib)
    4ms
    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 (ChiCTR2500105081)
    P4, N=5, Not yet recruiting, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine; Ruijin Hospital, Shanghai Jiao Tong University School of Medicine
    New P4 trial
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    BRAF (B-raf proto-oncogene)
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    BRAF V600E • BRAF V600 • BRAF positive
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    Erbitux (cetuximab) • Zelboraf (vemurafenib) • Kolupin (tunlametinib)
    4ms
    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.
    Journal • PD(L)-1 Biomarker • IO biomarker
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    NRAS (Neuroblastoma RAS viral oncogene homolog)
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    Kolupin (tunlametinib)
    6ms
    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 (ChiCTR2500102053)
    P2, N=38, Not yet recruiting, Peking Union Medical College Hospital; Peking Union Medical College Hospital
    New P2 trial
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    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
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    BRAF V600E • KRAS mutation • NRAS mutation • BRAF V600 • RAS mutation • NRAS Q61 • KRAS Q61
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    Fruzaqla (fruquintinib) • Kolupin (tunlametinib) • hydroxychloroquine
    7ms
    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, Fudan University
    New P2 trial
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    Kolupin (tunlametinib)
    7ms
    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.
    Journal • IO biomarker
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    NRAS (Neuroblastoma RAS viral oncogene homolog)
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    NRAS mutation
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    Mekinist (trametinib) • Kolupin (tunlametinib) • naporafenib (ERAS-254)
    9ms
    Efficacy and Safety of Tunlametinib Plus Vemurafenib in Patients With BRAF V600E-mutant Metastatic Colorectal Cancer (clinicaltrials.gov)
    P3, N=165, Recruiting, Shanghai Kechow Pharma, Inc. | Not yet recruiting --> Recruiting
    Enrollment open
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    BRAF (B-raf proto-oncogene)
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    BRAF V600E • BRAF V600
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    Avastin (bevacizumab) • Erbitux (cetuximab) • Zelboraf (vemurafenib) • Kolupin (tunlametinib)
    over1year
    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.
    Review • Journal • PD(L)-1 Biomarker • IO biomarker
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    NRAS (Neuroblastoma RAS viral oncogene homolog) • MAP2K1 (Mitogen-activated protein kinase kinase 1) • NF1 (Neurofibromin 1)
    |
    Kolupin (tunlametinib)
    over1year
    Comparing Tunlametinib Capsules and Combination Chemotherapy in Advanced NRAS-mutant Melanoma (clinicaltrials.gov)
    P3, N=165, Recruiting, Shanghai Kechow Pharma, Inc. | Not yet recruiting --> Recruiting
    Enrollment open • IO biomarker • Metastases
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    NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    cisplatin • carboplatin • paclitaxel • temozolomide • dacarbazine • Kolupin (tunlametinib)
    over1year
    Tunlametinib (HL-085) plus vemurafenib in patients with advanced BRAF V600-mutant solid tumors: an open-label, single-arm, multicenter, phase I study. (PubMed, Exp Hematol Oncol)
    Tunlametinib (HL-085) plus vemurafenib had a favorable safety profile and showed promising antitumor activity in patients with BRAF V600-mutant solid tumors. The RP2D for NSCLC was tunlametinib 9 mg BID plus vemurafeinib 720 mg BID.
    P1 data • Journal • Metastases
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    BRAF (B-raf proto-oncogene)
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    Zelboraf (vemurafenib) • Kolupin (tunlametinib)