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DRUG:

Kinaction (masitinib)

i
Other names: AB 1010, AB1010, AB-1010
Associations
Company:
AB Science
Drug class:
Multi-tyrosine kinase inhibitor, Macrophage inhibitor, Mast cell inhibitor, SARS-CoV-2 3CL pro inhibitor
Associations
3d
Macrophage-Derived PDGF-BB and GDF-15 Promote Drug Resistance in KRAS-Mutant Colorectal Cancer. (PubMed, bioRxiv)
In contrast, macrophage-conditioned medium had little effect on regorafenib and increased sensitivity to dabrafenib, suggesting that resistance depends on the inhibitory profile of each drug. The multi-kinase inhibitor masitinib-which targets several kinases along this resistance network-strongly restored sensitivity to trametinib and RMC-6236. Together, these data define a macrophage-driven resistance network in KRAS-mutant colorectal cancer organoids and support combined inhibition of RAS-pathway and tyrosine kinase signalling.
Journal
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KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • GDF15 (Growth differentiation factor 15)
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KRAS mutation
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Mekinist (trametinib) • Tafinlar (dabrafenib) • Stivarga (regorafenib) • daraxonrasib (RMC-6236) • Kinaction (masitinib)
4d
Trial suspension
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Kinaction (masitinib)
1m
Masitinib for the Treatment of Severe Mast Cell Activation Syndrome (clinicaltrials.gov)
P2, N=72, Active, not recruiting, AB Science | Not yet recruiting --> Active, not recruiting
Enrollment closed
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Kinaction (masitinib)
1m
Masitinib in Severe Indolent or Smoldering Systemic Mastocytosis Unresponsive to Optimal Symptomatic Treatment (clinicaltrials.gov)
P3, N=140, Active, not recruiting, AB Science | Not yet recruiting --> Active, not recruiting
Enrollment closed
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Kinaction (masitinib)
5ms
Comparative pathophysiology and molecular insights into cutaneous and non-cutaneous canine skin cancers: focus on melanoma, mast cell tumors, and squamous cell carcinoma. (PubMed, Front Immunol)
Tyrosine kinase inhibitors (TKIs), such as toceranib phosphate (Palladia) and masitinib, have demonstrated efficacy in MCTs...This review comprehensively synthesizes state-of-the-art literature on canine skin cancer, addressing pathophysiological mechanisms, diagnostic advancements, and emerging therapeutic strategies. In addition, this review aims to improve early detection, treatment outcomes, and enduring prognosis for affected canines by integrating recent findings into molecular oncology and comparative medicine.
Review • Journal • IO biomarker
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BRAF (B-raf proto-oncogene) • TP53 (Tumor protein P53) • NRAS (Neuroblastoma RAS viral oncogene homolog) • KIT (KIT proto-oncogene, receptor tyrosine kinase) • PTGS2 (Prostaglandin-Endoperoxide Synthase 2)
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TP53 mutation • BRAF mutation • NRAS mutation • KIT mutation
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Kinaction (masitinib)
7ms
Masitinib in Patients With Mild Alzheimer's Disease (clinicaltrials.gov)
P3, N=600, Not yet recruiting, AB Science | Trial completion date: Dec 2026 --> Dec 2029 | Trial primary completion date: Dec 2026 --> Dec 2028
Trial completion date • Trial primary completion date
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Kinaction (masitinib)
8ms
Efficacy and Safety of Masitinib Versus Placebo in the Treatment of ALS Patients (clinicaltrials.gov)
P3, N=495, Recruiting, AB Science | Trial completion date: Dec 2023 --> Dec 2027 | Trial primary completion date: Dec 2023 --> Dec 2027
Trial completion date • Trial primary completion date
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Kinaction (masitinib) • riluzole
8ms
MASIMS: Masitinib in the Treatment of Patients With Primary Progressive or Non-active Secondary Progressive Multiple Sclerosis (clinicaltrials.gov)
P3, N=800, Active, not recruiting, AB Science | Recruiting --> Active, not recruiting | Trial completion date: Dec 2025 --> Dec 2028 | Trial primary completion date: Dec 2025 --> Dec 2028
Enrollment closed • Trial completion date • Trial primary completion date
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Kinaction (masitinib)
9ms
Tyrosine Kinase Inhibitors for Gastrointestinal Stromal Tumor After Imatinib Resistance. (PubMed, Pharmaceutics)
Sunitinib, regorafenib, and ripretinib are currently approved as standard second-, third-, and fourth-line therapies, each demonstrating efficacy against distinct mutational profiles. Avapritinib, notably effective against PDGFRA D842V mutations, represents a milestone for previously untreatable subgroups. Several alternative agents-such as nilotinib, masitinib, sorafenib, dovitinib, pazopanib, and ponatinib-have shown varying degrees of success in refractory cases or specific genotypes. Investigational compounds, including crenolanib, bezuclastinib, famitinib, motesanib, midostaurin, IDRX-42, and olverembatinib, are under development to address resistant or wild-type GISTs...Future strategies include precision medicine approaches such as ctDNA-guided therapy, rational drug combinations, and novel drug delivery systems to optimize bioavailability and reduce toxicity. Ongoing research will be crucial for refining treatment sequencing and expanding therapeutic options, especially for rare GIST subtypes.
Review • Journal
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KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
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KIT mutation • PDGFRA D842V • PDGFRA mutation
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sorafenib • imatinib • sunitinib • Iclusig (ponatinib) • pazopanib • nilotinib • Stivarga (regorafenib) • midostaurin • crenolanib (ARO-002) • Ayvakit (avapritinib) • Nailike (olverembatinib) • Qinlock (ripretinib) • dovitinib (TKI258) • famitinib (SHR 1020) • motesanib (AMG 706) • bezuclastinib (PLX9486) • velzatinib (GSK6042981) • Kinaction (masitinib)