Ligand id: 7888

Name: apitolisib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 11
Hydrogen bond donors 2
Rotatable bonds 6
Topological polar surface area 162.07
Molecular weight 498.22
XLogP -1
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Apitolisib has been investigated in clinical trials for breast cancer, endometrial cancer, refractory solid tumours, Non-Hodgkin's lymphoma and other advanced solid tumours such as prostate cancer and renal cell cancer. Click here to link to ClinicalTrials.gov's listing of Phase II apitolisib trials.
Mechanism Of Action and Pharmacodynamic Effects
PI3Ks and mTOR participate in related, but not redundant, signaling networks to transmit cellular growth and survival signals, which are hallmarks of tumor growth [1,3-4]. Due to their active site similarity, dual PI3K/mTOR inhibitors have been intensely investigated as antineoplastic agents [2,6].