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    DRUG:

    Koselugo (selumetinib)

    i
    Other names: AZD6244, ARRY-886, AZD 6244 HydSulfate, ARRY-142886, NSC-748727, AZD-6244, MK-5618, AZD2644, AR00142886, ARRY142886, ARRY886, AZD142886, AR-00142886, ARRY 142886, ARRY 886, AZD-142886, AZD-2644, AZD 2644, AZD 6244, AZD 142886, MK 5618, AR 00142886, AR 142886 X
    Company:
    AstraZeneca, Merck (MSD), Pfizer
    Drug class:
    MEK inhibitor
    Related drugs:
    5d
    TATTON: AZD9291 in Combination With Ascending Doses of Novel Therapeutics (clinicaltrials.gov)
    P1, N=344, Active, not recruiting, AstraZeneca | Trial completion date: Dec 2025 --> Dec 2026
    Trial completion date
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M
    |
    Tagrisso (osimertinib) • Imfinzi (durvalumab) • Koselugo (selumetinib) • Orpathys (savolitinib) • simmitinib (SYHA1817)
    7d
    Inhibition of focal adhesion kinase impairs tumor formation and preserves hearing in a murine model of NF2-related schwannomatosis. (PubMed, Sci Adv)
    Pharmacological inhibition of FAK with single agent VS-4718 did not significantly reduce macroscopic tumor volume; however, its use in combination with the mitogen-activated protein kinase kinase (MEK) inhibitor selumetinib resulted in both a significant reduction in tumor volume and the preservation of dorsal root ganglion architecture. Our findings establish a critical role for FAK in schwannoma development and provide rationale for evaluation of combination FAK plus MEK inhibition in future clinical trials for NF2-associated SWN.
    Preclinical • Journal
    |
    HGF (Hepatocyte growth factor) • NF2 (Neurofibromin 2) • NLRC5 (NLR Family CARD Domain Containing 5) • PTK2 (Protein Tyrosine Kinase 2)
    |
    Koselugo (selumetinib) • VS-4718
    8d
    Integrating cuproptosis- and ferroptosis-related gene signatures to predict prognosis, immunotherapy response, and drug sensitivity in patients with skin cutaneous melanoma. (PubMed, Front Immunol)
    IFNG, PTPN6, SLC38A1, and SOCS1 may serve as potential biomarkers of poor prognosis in SKCM patients. These genes demonstrate predictive value for immunotherapy response and drug sensitivity, particularly indicating susceptibility to selumetinib treatment, and therefore show substantial potential for clinical translation.
    Journal • Gene Signature • IO biomarker
    |
    IFNG (Interferon, gamma) • SOCS1 (Suppressor Of Cytokine Signaling 1)
    |
    Koselugo (selumetinib)
    10d
    Pharmacokinetics and Safety of Selumetinib Granule Formulation in Children With Symptomatic, Inoperable Neurofibromatosis Type 1-Related Plexiform Neurofibromas (SPRINKLE; phase I/II). (PubMed, J Clin Oncol)
    Selumetinib granule formulation (25 mg/m2 dose equivalent, twice a day) had comparable exposure to selumetinib capsule formulation, and was palatable with a manageable safety profile. Selumetinib granule formulation is potentially suitable for young children with NF1-PN who cannot swallow capsules.
    P1/2 data • PK/PD data • Journal
    |
    NF1 (Neurofibromin 1)
    |
    Koselugo (selumetinib)
    15d
    A Phase 2 Study of Osimertinib in Combination With Selumetinib in EGFR Inhibitor naïve Advanced EGFR Mutant Lung Cancer (clinicaltrials.gov)
    P2, N=25, Active, not recruiting, Dana-Farber Cancer Institute | Trial completion date: Jun 2026 --> Dec 2026 | Trial primary completion date: Dec 2025 --> Jun 2026
    Trial completion date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion
    |
    Tagrisso (osimertinib) • Koselugo (selumetinib) • simmitinib (SYHA1817)
    21d
    Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial) (clinicaltrials.gov)
    P2, N=1376, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: May 2026 --> Jan 2027
    Trial completion date
    |
    BRAF (B-raf proto-oncogene)
    |
    Lynparza (olaparib) • Ibrance (palbociclib) • Zelboraf (vemurafenib) • Vitrakvi (larotrectinib) • Koselugo (selumetinib) • Balversa (erdafitinib) • Retevmo (selpercatinib) • Ensacove (ensartinib) • Zarnestra (tipifarnib) • Tibsovo (ivosidenib) • Tazverik (tazemetostat) • ulixertinib (BVD-523) • samotolisib (LY3023414)
    29d
    SARC031: A Phase 2 Trial of Selumetinib and Sirolimus for Patients with Unresectable or Metastatic Malignant Peripheral Nerve Sheath Tumors (MPNST). (PubMed, Clin Cancer Res)
    The combination was safe with manageable and expected AEs, but did not meet study parameters for further evaluation in MPNST. Correlative studies were informative and may guide future therapeutic trials of MPNST.
    P2 data • Journal
    |
    NF1 (Neurofibromin 1)
    |
    Koselugo (selumetinib) • sirolimus
    1m
    Targeted therapies in optic pathway gliomas. (PubMed, Cancer Treat Rev)
    Targeted therapies constitute a potentially paradigm-shifting development in the management of OPGs, enhancing disease control while improving the prospects for long-term visual preservation. This review underscores the need for individualized, biomarker-driven approaches and highlights challenges including resistance, long-term safety, and therapy duration.
    Review • Journal
    |
    NF1 (Neurofibromin 1)
    |
    Koselugo (selumetinib)
    1m
    Selumetinib and Azacitidine in High Risk Chronic Blood Cancers (clinicaltrials.gov)
    P1, N=18, Recruiting, University of Chicago | Trial completion date: Sep 2025 --> Sep 2027 | Trial primary completion date: Sep 2025 --> Sep 2027
    Trial completion date • Trial primary completion date
    |
    Koselugo (selumetinib) • azacitidine
    1m
    Real-World Treatment Study of Koselugo (Selumetinib) (clinicaltrials.gov)
    P=N/A, N=200, Recruiting, AstraZeneca | N=150 --> 200
    Enrollment change • HEOR • Real-world evidence
    |
    Koselugo (selumetinib)
    2ms
    Transcriptome-guided drug repurposing identifies selumetinib for an aggressive epithelial cancer. (PubMed, J Invest Dermatol)
    RNA sequencing identified early growth response protein 1 (EGR1), fos proto-oncogene (FOS), and dual-specificity phosphatase 6 (DUSP6) as candidate biomarkers of treatment response. Selumetinib, identified by computational drug screening, demonstrates efficacy against RDEB-SCCs in vitro and in vivo, suggesting its potential for clinical use.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • CDH1 (Cadherin 1) • VIM (Vimentin) • DUSP6 (Dual specificity phosphatase 6) • EGR1 (Early Growth Response 1)
    |
    Koselugo (selumetinib)
    2ms
    SPRINKLE: Pharmacokinetics, Safety and Efficacy of the Selumetinib Granule Formulation in Children Aged ≥1 to <7 Years With NF1-related Symptomatic, Inoperable PN (clinicaltrials.gov)
    P1/2, N=36, Active, not recruiting, AstraZeneca | Trial primary completion date: Apr 2024 --> Nov 2027
    Trial primary completion date
    |
    NF1 (Neurofibromin 1)
    |
    Koselugo (selumetinib)