| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H25ClFN5O3 |
| Molecular Weight | 473.928 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CNC(=O)CN1CCC(CC1)OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC
InChI
InChIKey=DFJSJLGUIXFDJP-UHFFFAOYSA-N
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)
| Molecular Formula | C23H25ClFN5O3 |
| Molecular Weight | 473.928 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Sapitinib is an oral, reversible and equipotent inhibitor of EGFR, HER2 and HER3 signalling. The drug was tested in phase II of clinical trials in patients with breast cancer, colorectal cancer, gastric cancer and NSCL carcinoma, however its development for breast cancer therapy seems to be terminated. Sapitinib absorption is rapid and the drug is totally cleared by metabolism with the major routes being oxidation and amine or ether cleavage around the piperidine ring with subsequent glucuronide or sulphate conjugation.
CNS Activity
Originator
Approval Year
Sourcing
PubMed
Sample Use Guides
Colorectal cancer: Patients were receiving 160 mg sapitinib tablets, twice daily on days 1-4 of each 2-weekly cycle + FOLFIRI. Breast cancer: Patients were receiving daily anastrozole (1 mg) in combination with sapitinib 20 mg twice daily (bid) or sapitinib 40 mg bid.
Route of Administration:
Oral
