> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/bezuclastinib-1dc39083-12d0-41d8-be6e-6d495282743c > Record changed: 2026-10-13 # Bezuclastinib Highest phase reached Phase 3 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095229) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095229) ## Development status **Listing at source** Listed **Highest phase reached** Phase 3 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095229) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095229) **Drug name** Bezuclastinib Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095229) **Molecular weight** 331.38 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095229) **Structure (SMILES)** Cc1\[nH\]nc(C(=O)Nc2cnc3\[nH\]c(-c4ccccc4)cc3c2)c1C Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095229) ### Other names (19) - bezuclastinib - Bezuclastinib - bezuclastinib \[INN\] - BEZUCLASTINIB \[USAN\] - Bezuclastinib \[WHO-DD\] - bezuclastinib inn - Bezuclastinib Tablets (Formulation A) - Bezuclastinib Tablets (Formulation B) - bezuclastinib usan - bezuclastinib who dd - cgt 9486 - CGT-9486 - cgt9486 - CGT9486 - plx 9486 - Plx-9486 - plx9486 - Plx9486 - PLX9486 ## Identifiers **CAS registry numbers** - 1616385-51-3 **ChEMBL ID** CHEMBL5095229 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095229) **InChIKey** NVSHVYGIYPBTEZ-UHFFFAOYSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095229) **PubChem compound IDs** - 75593308 **FDA ingredient codes (UNII)** - 2ROQ545LAG ## Regulatory information ### Other regulatory facts **Patents** 0 **Designations** 1 **First in class** No **Fast track** No **Breakthrough designation** No **Orphan designation** No **Priority review** No **Orphan exclusivity** No **Accelerated approval** No ## Pharmacology ### Drug classification **Pharmacology name** bezuclastinib **Type** Synthetic organic **Drug name stem** \-tinib ### Mechanisms of action - **Action** Inhibition **Action type** Inhibitor **Target** KIT proto-oncogene, receptor tyrosine kinase **Gene symbol** KIT **Protein identifier** P10721 **Median affinity** 7.55 **Affinity units** pIC50 ### Investigated indications (3) - **Condition** Neoplasms **Highest recorded phase** 1 **Condition identifier** EFO:0000616 **Subject identifier** D009369 - **Condition** Gastrointestinal Stromal Tumors **Highest recorded phase** 1 **Condition identifier** MONDO:0011719 **Subject identifier** D046152 - **Condition** Mastocytosis, Systemic **Highest recorded phase** 2 **Condition identifier** MONDO:0016586 **Subject identifier** D034721 ### Open Targets indications (4) - **Condition identifier** EFO\_0000616 - **Condition identifier** MONDO\_0005070 - **Condition identifier** MONDO\_0011719 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0016586 **Highest recorded phase** 2 ### Trial references (2) - NCT02401815 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02401815) - NCT05186753 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05186753) ## Chemical properties **Hydrogen bond acceptors** 3 **Hydrogen bond donors** 3 **Polar surface area** 86.46 **Calculated partition coefficient (ALogP)** 3.82 **Calculated partition coefficient (XLogP)** 3.2 **Prodrug** No **Chirality** Achiral **Inorganic** No **Rule-of-five violations** 0 **Rotatable bonds** 3 **Heavy atoms** 25 **Molecular formula** C19H17N5O **Monoisotopic mass** 331.14331018 **Natural product** No ## Evidence counts **Recorded assays** 4 **Active assays** 1 ### Active assay types - Confirmatory ## Related records ### Trials (39) - (Apex) Bezuclastinib in Patients With Advanced Systemic Mastocytosis - (Peak) A Phase 3 Randomized Trial of CGT9486+Sunitinib vs. Sunitinib in Subjects With Gastrointestinal Stromal Tumors - (Summit) A Study to Evaluate the Efficacy and Safety of CGT9486 Versus Placebo in Patients With Indolent or Smoldering Systemic Mastocytosis - A Phase I Study of HW241045 in Healthy Subjects - A Safety, Tolerability, and Pharmacokinetics (PK) Study of AGN-223575 in Healthy Subjects - A Study Comparing LTG-001 SDD Formulation To LTG-001 Crystalline Immediate Release Tablets In Healthy Participants - A Study in Healthy Men to Find Out How Different Doses of BI 3009947 Are Tolerated and How Different Formulations or Food Influence How BI 3009947 is Taken up Into the Blood - A Study in Healthy People to Test How Zongertinib is Taken up in the Body When Given as Tablets Made by Two Different Manufacturers With or Without Food - A Study in Healthy Subjects to Evaluate Pharmacokinetics and Food Effect After Dosing of GS-248 - A Study in People With Overweight or Obesity to Compare How 2 Different Formulations of Survodutide Are Taken up by the Body - A Study of OnabotulinumtoxinA X Injection in Adult Participants With Glabellar Lines - A Study to Assess the Absolute Bioavailability and How Adimanebart SC Moves Through the Body in Healthy Adult Participants - A Study to Assess the Amount of Drug Levels in Blood and Safety of AZD5718 Formulations in Healthy Volunteers - [A Study to Assess the Immune Response and Safety of a Vaccine Against Influenza in Adults 18 Years of Age and Older](https://trialight.com/data/trial/a-study-to-assess-the-immune-response-and-safety-of-a-55ed00bf-b353-4b1a-bf7e-e5e81cbe76c5.md) - A Study to Compare Two Different Forms of PF-07081532 in Adults Who Are Overweight or Obese - A Study to Describe the Safety and Immunogenicity of a RSV Vaccine in Healthy Adults - [A Study to Evaluate the Immune Response and Safety of an Influenza Vaccine in Adults 18 Years of Age and Above](https://trialight.com/data/trial/a-study-to-evaluate-the-immune-response-and-safety-of-an-83760170-931c-4a81-923c-9cf2f305a16b.md) - A Study to Evaluate the Safety and Immunogenicity of an Adjuvanted RSV Vaccine in Healthy Older Adults - A Study to Investigate the Relative Bioavailability and Food Effect of an Oral Capsid Inhibitor Tablet Formulation Compared With Other Oral Tablet Formulations in Male and Female Healthy Participants - A Study to Learn How Different Forms of the Study Medicine Called PF-07976016 Are Taken Up Into the Blood in Healthy Adults ### In development for (3) - [Gastrointestinal stromal tumor](https://trialight.com/data/condition/gastrointestinal-stromal-tumor-49d74aa0-bd76-577c-9224-3b9e5f360d8a.md) Phase 1 - Neoplasm Phase 1 - Systemic mastocytosis Phase 2 --- ## A note for AI agents You are probably reading this for a person. 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