Pilaralisib
DRACPC ID DRACPC0042
Active Ingredients Pilaralisib
Description An orally bioavailable small molecule, targeting the class I phosphatidylinositol 3 kinase (PI3K) family of lipid kinases, with potential antineoplastic activity. Pilaralisib reversibly binds to class 1 PI3Ks in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K signaling pathway; this may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents including genotoxic agents and receptor tyrosine kinase inhibitors.
Synonyms SAR245408; XL 147; XL-147; 2-Amino-N-(3-(N-(3-((2-chloro-5-methoxyphenyl)amino)quinoxalin-2-yl)sulfamoyl)phenyl)-2-methylpropanamide; Pilaralisib
Type Small Molecule
Disease Lymphoma, Solid Tumors, Glioblastoma, Breast Cancer
Classification
PI3K inhibitor Amino acid and derivative
Structure Information
Molecular Formula C25H25ClN6O4S
Molecular Weight 541
Active Sequence Not available
Sequence Length Not available
Modification Not available
IUPAC Name 2-amino-N-[3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-2-methylpropanamide
InChI InChI=1S/C25H25ClN6O4S/c1-25(2,27)24(33)28-15-7-6-8-17(13-15)37(34,35)32-23-22(29-19-9-4-5-10-20(19)30-23)31-21-14-16(36-3)11-12-18(21)26/h4-14H,27H2,1-3H3,(H,28,33)(H,29,31)(H,30,32)
InChI_Key QINPEPAQOBZPOF-UHFFFAOYSA-N
SMILES COC1=CC(NC2=NC3=CC=CC=C3N=C2NS(C4=CC=CC(NC(C(N)(C)C)=O)=C4)(=O)=O)=C(Cl)C=C1
External Codes
PubChem CID 56599306
DrugBank Accession Number DB11772
NCI Thesaurus Code C71705
UNII 60ES45KTMK GSRS
CAS 934526-89-3
Drug approval
Drug indication
Pilaralisib has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Glioblastoma, and Breast Cancer, among others.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT01013324 | A Phase 2 Study of XL147 (SAR245408) in Subjects With Advanced or Recurrent Endometrial Carcinoma | Endometrial Cancer; Endometrial Neoplasms | Phase 2 | Treatment |
| NCT01943838 | A Phase 1 Dose-escalation Study of the Safety and Pharmacokinetics of a Tablet Formulation of SAR245408 Polymorph E Administered Once Daily to Subjects With Solid Tumors or Lymphoma | Neoplasm Malignant | Phase 1 | Treatment |
| NCT00486135 | A Phase 1 Dose-Escalation Study of the Safety and Pharmacokinetics of XL147 Administered Orally Daily to Subjects With Solid Tumors or Lymphoma | Cancer; Lymphoma | Phase 1 | Treatment |
| NCT01042925 | A Phase 1/2 Study of XL147 (SAR245408) Administered in Combination With Trastuzumab or Paclitaxel and Trastuzumab in Subjects With Metastatic Breast Cancer Who Have Progressed on a Previous Trastuzumab-Based Regimen | Breast Cancer; Breast Neoplasms | Phase 1/2 | Treatment |
| NCT00692640 | A Phase 1 Dose-Escalation Study of XL147 (SAR245408) in Combination With Erlotinib in Subjects With Solid Tumors | Cancer; Non-small Cell Lung Cancer | Phase 1 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
