^
    7d
    Properties of FDA-approved small molecule protein kinase inhibitors: a 2026 update. (PubMed, Pharmacol Res)
    The following ten drugs received FDA approval in 2025 - avutometinib (inhibiting MEK1/2 in serous ovarian carcinomas), defactinib (blocking FAK in low grade serous ovarian carcinomas), delgocitinib (antagonizing the JAK family in hand eczema), mirdametinib (inhibiting MEK1/2 in type I neurofibromatosis), remibrutinib (blocking BTK in chronic spontaneous urticaria), rilzabrutinib (antagonizing BTK in chronic immune thrombocytopenia), sunvozertinib (blocking mutant exon 21 insertion EGFR NSCLC), taletrectinib (inhibiting mutant ROS1 in NSCLC), vimseltinib (blocking CSF1R in tenosynovial giant cell tumors), and zongertinib (antagonizing mutant HER2 in NSCLC). This article summarizes the physicochemical properties of all 94 FDA-approved small molecule protein kinase inhibitors including the molecular weight, number of hydrogen bond donors/acceptors, ligand efficiency, lipophilic efficiency, polar surface area, and solubility. A total of 45 of the 94 FDA-approved drugs have a least one Lipinski rule of five violation.
    FDA event • Review • Journal
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    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • CSF1R (Colony stimulating factor 1 receptor)
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    EGFR mutation
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    Gomekli (mirdametinib) • Avmapki (avutometinib) • Hernexeos (zongertinib) • Fakzynja (defactinib) • Ibtrozi (taletrectinib) • Zegfrovy (sunvozertinib) • Rhapsido (remibrutinib) • Romvimza (vimseltinib)
    10d
    Downregulation of SLC12A5 in glioblastoma multiforme: a novel prognostic biomarker associated with brain edema and radiomic features. (PubMed, Naunyn Schmiedebergs Arch Pharmacol)
    Drug sensitivity screening identified six small molecules (PD0325901, ERK-6604, paclitaxel, ribociclib, TAF1, and lapatinib) that targeted SLC12A5-related pathways. Crucially, multivariate Cox regression analysis confirmed that SLC12A5 was an independent prognostic factor (HR p = 0.04). This study established SLC12A5 as a novel biomarker for GBM, uniquely bridging molecular dysregulation, edema pathogenesis, and radiomics with implications for prognosis and targeted therapy.
    Journal
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    SERPINH1 (Serpin family H member 1) • LOX (Lysyl Oxidase) • MMP9 (Matrix metallopeptidase 9) • VSNL1 (Visinin Like 1) • TAF1 (TATA-Box Binding Protein Associated Factor 1)
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    paclitaxel • lapatinib • Kisqali (ribociclib) • Gomekli (mirdametinib)
    10d
    Chromobox2 inhibition: a novel activity of alisertib, an aurora A kinase inhibitor. (PubMed, Mol Cancer Ther)
    In vitro validation narrowed compounds of interest to raltitrexed, alisertib, GTX-007, LY315920, and PD0325901. Treatment with alisertib leads to decrease in H2AK119ub and shift in the immune tumor microenvironment. Alisertib efficacy in HGSC is dependent on functional CBX2 and cell target engagement confirms selectivity for CBX2, supporting that alisertib activity involves CBX2 inhibition.
    Journal
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    AURKA (Aurora kinase A) • CBX2 (Chromobox 2)
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    Gomekli (mirdametinib) • alisertib (MLN8237) • Tomudex (raltitrexed)
    17d
    MIRV: Phase 1/2 Study of Mirdametinib + Vinblastine for Newly Diagnosed/Previously Untreated PLGG + Activation of MAPK (clinicaltrials.gov)
    P1/2, N=50, Recruiting, St. Justine's Hospital | Not yet recruiting --> Recruiting
    Enrollment open
    |
    BRAF (B-raf proto-oncogene) • NF1 (Neurofibromin 1) • KIAA1549
    |
    BRAF V600E • BRAF V600 • BRAF fusion
    |
    Gomekli (mirdametinib) • vinblastine
    26d
    A Window of Opportunity Trial of Mirdametinib Plus Vorinostat for NF1 Associated, H3K27 Trimethylation Deficient Malignant Peripheral Nerve Sheath Tumor [MPNST] (clinicaltrials.gov)
    P1, N=8, Recruiting, University of Minnesota | Trial completion date: Jan 2026 --> Jan 2027 | Trial primary completion date: Jan 2026 --> Jan 2027
    Trial completion date • Trial primary completion date
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    Gomekli (mirdametinib) • Zolinza (vorinostat)
    26d
    Study of the Safety and Pharmacokinetics of BGB-283 (Lifirafenib) and PD-0325901 (Mirdametinib) in Participants With Advanced or Refractory Solid Tumors (clinicaltrials.gov)
    P1, N=91, Completed, BeiGene | Trial completion date: Feb 2026 --> Oct 2025 | Active, not recruiting --> Completed
    Trial completion • Trial completion date
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    NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation
    |
    Gomekli (mirdametinib) • lifirafenib (BGB-283)
    27d
    Head-to-head preclinical treatment design prioritizes promising therapies for neurofibromatosis type 1 optic glioma clinical translation. (PubMed, Neurooncol Adv)
    Nf1 OPG mice were treated with standard of care (SOC; carboplatin), clinically evaluated (everolimus, mirdametinib), and investigational (pexidartinib, HBS-101, lamotrigine) drugs during the period of most rapid tumor growth (6-12 weeks of age). This referential preclinical study design affords direct head-to-head comparisons of investigational therapies relative to SOC treatment using clinically meaningful outcomes (OPG growth and RNFL thickness). Using this strategy, lamotrigine emerged as the most promising therapy for limiting tumor progression and vision loss in Nf1-OPG mice, relevant to clinical translation for children with NF1-OPG.
    Preclinical • Journal • Head-to-Head
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    NF1 (Neurofibromin 1) • CCL2 (Chemokine (C-C motif) ligand 2) • CCL3 (C-C Motif Chemokine Ligand 3)
    |
    carboplatin • everolimus • Gomekli (mirdametinib) • Turalio (pexidartinib)
    27d
    High-throughput drug screening identifies EGFR/MAPK pathway targeting sensitivities in organoid models of ovarian carcinosarcoma. (PubMed, J Exp Clin Cancer Res)
    OCS is the most aggressive, drug-resistant gynaecological malignancy and eribulin-based combination therapies, particularly triple combination therapies, have the potential to improve patient outcomes.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • HMGA2 (High mobility group AT-hook 2)
    |
    TP53 mutation • KRAS mutation • EGFR mutation
    |
    cisplatin • erlotinib • Halaven (eribulin mesylate) • Gomekli (mirdametinib)
    1m
    Testing the Effectiveness of the Anti-cancer Drug, Mirdametinib, in Treating Relapsed, Refractory Chronic Lymphocytic Leukemia (clinicaltrials.gov)
    P2, N=20, Recruiting, National Cancer Institute (NCI) | Not yet recruiting --> Recruiting | Initiation date: Jan 2026 --> Sep 2026
    Enrollment open • Trial initiation date
    |
    Gomekli (mirdametinib)
    2ms
    To Assess the Enzyme Inducing Effects of Carbamazepine on the PK of Mirdametinib in Healthy Participants (clinicaltrials.gov)
    P1, N=36, Not yet recruiting, SpringWorks Therapeutics, Inc.
    New P1 trial
    |
    Gomekli (mirdametinib)
    2ms
    Testing the Effectiveness of the Anti-cancer Drug, Mirdametinib, in Treating Relapsed, Refractory Chronic Lymphocytic Leukemia (clinicaltrials.gov)
    P2, N=20, Not yet recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2027 --> Feb 2030 | Trial primary completion date: Dec 2027 --> Feb 2030
    Trial completion date • Trial primary completion date
    |
    Gomekli (mirdametinib)