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

Structure

 

Show IUPAC/InChI/SMILES

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.





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