| Stereochemistry | ABSOLUTE |
| Molecular Formula | C25H30N6O3 |
| Molecular Weight | 462.5441 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CNC(=O)C1=CC=CC(=C1)C2=NC3=C(C=C2)C(=NC(=N3)N4CCOC[C@@H]4C)N5CCOC[C@@H]5C
InChI
InChIKey=JUSFANSTBFGBAF-IRXDYDNUSA-N
InChI=1S/C25H30N6O3/c1-16-14-33-11-9-30(16)23-20-7-8-21(18-5-4-6-19(13-18)24(32)26-3)27-22(20)28-25(29-23)31-10-12-34-15-17(31)2/h4-8,13,16-17H,9-12,14-15H2,1-3H3,(H,26,32)/t16-,17-/m0/s1
Vistusertib (AZ-2014) is a dual inhibitor of mTORC1/mTORC2 which was developed by AstraZeneca for the treatment of cancer. The drug is under clinical development (phase II) in patients with Renal Carcinoma, Squamous Non Small Cell Lung Cancer, Diffuse Large B-Cell Lymphoma, Meningioma, Breast cancer and Gastric cancer, either alone or in combination therapy. Vistusertib penetrates blood-brain barrier.
CNS Activity
Originator
Approval Year
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
Drug as perpetrator
Drug as victim
Tox targets
Sourcing
PubMed
Patents
Sample Use Guides
Renal Carcinoma: patients receive 50mg twice a day. Squamous Non Small Cell Lung Cancer: patients receive study treatment consisting of a single weekly paclitaxel infusion (80 mg/m2) on Day 1 of each week and twice daily 50 mg doses of vistusertib on the first 3 days each week for 6 weeks. Diffuse Large B-Cell Lymphoma: patients receive 125mg of vistusertib twice daily - 2 days on 5 days off in a 28 day cycle. Gastric Adenocarcinoma: patients receive 50mg of vistusertib twice dayly, 3 days on 4 days off of a 7 day cycle + paclitaxel 80mg/m2 given days 1, 8 and 15 of a 28 day cycle.
Route of Administration:
Oral
ACTIVE MOIETY
