Sapitinib
DRACPC ID DRACPC0004
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
Type Small Molecule
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
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.
