Elenestinib

Elenestinib
Clinical data
Other names	BLU-263
Legal status
Legal status	investigational;
Identifiers
	IUPAC name 2-[4-[4-[4-[5-[(1S)-1-amino-1-(4-fluorophenyl)ethyl]pyrimidin-2-yl]piperazin-1-yl]pyrrolo[2,1-f][1,2,4]triazin-6-yl]pyrazol-1-yl]ethanol;
CAS Number	2505078-08-8;
PubChem CID	155190269;
IUPHAR/BPS	12357;
DrugBank	DB18489;
ChemSpider	123963172;
UNII	6FBM4CP6RK;
KEGG	D12450;
ChEBI	CHEBI:759252;
ChEMBL	ChEMBL5314552;
Chemical and physical data
Formula	C27H29FN10O
Molar mass	528.596 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@](C1=CC=C(C=C1)F)(C2=CN=C(N=C2)N3CCN(CC3)C4=NC=NN5C4=CC(=C5)C6=CN(N=C6)CCO)N;
	InChI InChI=InChI=1S/C27H29FN10O/c1-27(29,21-2-4-23(28)5-3-21)22-14-30-26(31-15-22)36-8-6-35(7-9-36)25-24-12-19(17-38(24)34-18-32-25)20-13-33-37(16-20)10-11-39/h2-5,12-18,39H,6-11,29H2,1H3/t27-/m0/s1; Key:IPMARPMXSFFZFG-MHZLTWQESA-N;

Elenestinib is an investigational new drug that is being evaluated by Blueprint Medicines (a Sanofi company) for the treatment of indolent and smoldering systemic mastocytosis (SM), a rare disease where excess abnormal mast cells build up in internal organs, causing allergy‑like symptoms and organ damage. It is an inhibitor of the proto-oncogene c-kit protein harboring the D816V SM driver mutation.^[1]^[2]

Clinical trials

Elenestinib is in phase 3 clinical trials for systemic mastocytosis.^[3]

References

↑ "Elenestinib - Blueprint Medicines". AdisInsight. Springer Nature Switzerland AG.
↑ Valent P, Hartmann K, Stefanzl G, Filik Y, Bauer K, Degenfeld-Schonburg L, et al. (February 2026). "Systemic Mastocytosis, KIT and the Effects of KIT Tyrosine Kinase Inhibitors on Mast Cell and Basophil Activation". Current Allergy and Asthma Reports. 26 (1) 10. doi:10.1007/s11882-026-01257-6. PMC 12913350. PMID 41701410.
↑ Clinical trial number NCT04910685 for "(HARBOR) Study to Evaluate Efficacy and Safety of BLU-263 Versus Placebo in Patients With Indolent Systemic Mastocytosis" at ClinicalTrials.gov

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[AdisInsight-1] "Elenestinib - Blueprint Medicines". AdisInsight. Springer Nature Switzerland AG.

[pmid41701410-2] Valent P, Hartmann K, Stefanzl G, Filik Y, Bauer K, Degenfeld-Schonburg L, et al. (February 2026). "Systemic Mastocytosis, KIT and the Effects of KIT Tyrosine Kinase Inhibitors on Mast Cell and Basophil Activation". Current Allergy and Asthma Reports. 26 (1) 10. doi:10.1007/s11882-026-01257-6. PMC 12913350. PMID 41701410.

[3] Clinical trial number NCT04910685 for "(HARBOR) Study to Evaluate Efficacy and Safety of BLU-263 Versus Placebo in Patients With Indolent Systemic Mastocytosis" at ClinicalTrials.gov

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Clinical trials

References