Pexidartinib hydrochlorideProduct ingredient for Pexidartinib
- Name
- Pexidartinib hydrochloride
- Drug Entry
- Pexidartinib
Pexidartinib is a selective tyrosine kinase inhibitor that works by inhibiting the colony-stimulating factor (CSF1)/CSF1 receptor pathway. Pexidartinib was originally developed by Daiichi Sankyo, Inc. and it was approved by the FDA in August 2019 as the first systemic therapy for adult patients with symptomatic tenosynovial giant cell tumor.11 Tenosynovial giant cell tumor is a rare form of non-malignant tumor that causes the synovium and tendon sheaths to thicken and overgrow, leading to damage in surrounding joint tissue.1,11 Debilitating symptoms often follow with tenosynovial giant cell tumors, along with a risk of significant functional limitations and a reduced quality of life in patients.11
While surgical resection is a current standard of care for tenosynovial giant cell tumor, there are tumor types where surgeries are deemed clinically ineffective with a high risk of lifetime recurrence.10 Pexidartinib works by blocking the immune responses that are activated in tenosynovial giant cell tumors. In clinical trials, pexidartinib was shown to promote improvements in patient symptoms and functional outcomes in TGCT.2 Pexidartinib is available in oral formulations and it is commonly marketed as Turalio.11
- Accession Number
- DBSALT002881
- Structure
- Synonyms
- Pexidartinib HCl / Pexidartinib hydrochloride
- External IDs
- FP-113
- UNII
- YS6WAI3XN7
- CAS Number
- 2040295-03-0
- Weight
- Average: 454.28
Monoisotopic: 453.0734854 - Chemical Formula
- C20H16Cl2F3N5
- InChI Key
- CJLUYLRKLUYCEK-UHFFFAOYSA-N
- InChI
- InChI=1S/C20H15ClF3N5.ClH/c21-15-6-16-14(10-28-19(16)29-11-15)5-12-2-4-18(26-7-12)27-9-13-1-3-17(25-8-13)20(22,23)24;/h1-4,6-8,10-11H,5,9H2,(H,26,27)(H,28,29);1H
- IUPAC Name
- 5-({5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl}methyl)-N-{[6-(trifluoromethyl)pyridin-3-yl]methyl}pyridin-2-amine hydrochloride
- SMILES
- Cl.FC(F)(F)C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C34)C=C2)C=N1
- External Links
- ChemSpider
- 64853817
- ChEMBL
- CHEMBL3989973
- Predicted Properties
Property Value Source Water Solubility 0.00315 mg/mL ALOGPS logP 4.64 ALOGPS logP 4.54 Chemaxon logS -5.1 ALOGPS pKa (Strongest Acidic) 15.68 Chemaxon pKa (Strongest Basic) 6.76 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 66.49 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 105.89 m3·mol-1 Chemaxon Polarizability 39.33 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon