Sapitinib

DCTPepD ID  DCTPepD0004

Active Ingredients   Sapitinib

Description  An erbB receptor tyrosine kinase inhibitor with potential antineoplastic activity. erbB kinase inhibitor AZD8931 binds to and inhibits erbB tyrosine receptor kinases, which may result in the inhibition of cellular proliferation and angiogenesis in tumors expressing erbB. The erbB protein family, also called the epidermal growth factor receptor (EGFR) family, plays major roles in tumor cell proliferation and tumor vascularization.

Synonyms  AZD8931; AZD-8931; 2-(4-((4-((3-Chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)-n-methylacetamide; ErbB Kinase Inhibitor AZD8931; Sapitinib

Disease  Breast cancer, Metastatic cancer

Classification

  

ErbB Kinase Inhibitor Amino acid and derivative

Structure Information


Molecular Formula  C23H25ClFN5O3

Molecular Weight  473.9

Active Sequence  Not available

Sequence Length  Not available

Modification  None

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  2-[4-[4-(3-chloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]-N-methylacetamide

InChI  InChI=1S/C23H25ClFN5O3/c1-26-21(31)12-30-8-6-14(7-9-30)33-20-10-15-18(11-19(20)32-2)27-13-28-23(15)29-17-5-3-4-16(24)22(17)25/h3-5,10-11,13-14H,6-9,12H2,1-2H3,(H,26,31)(H,27,28,29)

InChI_Key DFJSJLGUIXFDJP-UHFFFAOYSA-N

SMILES  CNC(CN1CCC(OC2=C(OC)C=C3C(C(NC4=C(F)C(Cl)=CC=C4)=NC=N3)=C2)CC1)=O

External Codes


PubChem CID  11488320

DrugBank Accession Number  DB12183

NCI Thesaurus Code  C77887  

UNII  3499328002   GSRS

CAS  848942-61-0



Drug approval


Drug indication
    Sapitinib has been used in trials studying the treatment and basic science of Neoplasms, Breast Cancer, Breast Neoplasms, Metastatic Cancer, and Metastatic Breast Cancer, among others.

    The drug is not approved.

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT01862003 AZD8931, an Inhibitor of EGFR, ERBB2 and ERBB3 Signalling, in Combination With FOLFIRI: a Phase I/II Study to Determine the Importance of Schedule and Activity in Colorectal Cancer Metastatic Colorectal Cancer; Recurrent Colorectal Cancer Phase 2 Treatment
NCT01596530 A Randomised Double-Blind Placebo-controlled Multicentre Phase I Study to Assess the Biological Activity of AZD8931 in Patients With Early Breast Cancer Who Are Ineligible for Treatment With Trastuzumab as Defined by IHC Status Breast Neoplasm Phase 1 Treatment
NCT01003158 A Phase I, Open-label, Multiple-dose, Dose-escalation Study To Assess the Safety and Tolerability of AZD8931 Monotherapy in Japanese Patients With Advanced Solid Malignancies and in Combination With Paclitaxel in Japanese Female Patients With Advanced Breast Cancer Neoplasms; Metastatic Cancer; Breast Cancer Phase 1 Treatment
NCT00900627 A Phase I/II Multi-centre Study of AZD8931 in Combination With Weekly Paclitaxel to Assess the Safety, Tolerability, Pharmacokinetics and Efficacy in Patients With Advanced Solid Tumours and in a Selected Population With Low HER2-expressing Locally Recurrent and/or Metastatic Breast Cancer Neoplasms; Breast Neoplasms; Breast Cancer Phase 1/2 Treatment
NCT00637039 A Phase 1, Open-label, Multiple-dose, Dose Escalation Study to Assess the Safety, Tolerability and Pharmacokinetics of AZD8931 in Patients With Advanced Solid Malignancies Advanced Solid Malignancies Phase 1 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





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