Rucha Sane
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View article: Pharmacokinetics, safety and tolerability of ipatasertib in combination with palbociclib and fulvestrant in patients with advanced breast cancer in a phase Ib study
Pharmacokinetics, safety and tolerability of ipatasertib in combination with palbociclib and fulvestrant in patients with advanced breast cancer in a phase Ib study Open
Introduction Ipatasertib is a potent, highly selective, small molecule AKT inhibitor that has been evaluated in combination with palbociclib and fulvestrant for the treatment of hormone receptor-positive (HR+) human epidermal growth factor…
View article: Quantifying Risk of Delayed QT Prolongation of Ipatasertib in Preclinical and Clinical Studies in Cancer Patients
Quantifying Risk of Delayed QT Prolongation of Ipatasertib in Preclinical and Clinical Studies in Cancer Patients Open
QTc prolongation has been associated with torsades de pointes (TdP) and also with other cardiac diseases. We investigated the effect of ipatasertib, a selective serine/threonine kinase (AKT, protein kinase B) inhibitor, on preclinical mode…
View article: Impact of P‐gp inhibition on systemic exposure of pralsetinib and dosing considerations
Impact of P‐gp inhibition on systemic exposure of pralsetinib and dosing considerations Open
A study to determine the impact of cyclosporine (Neoral), an inhibitor of P‐gp, on the pharmacokinetics of pralsetinib (trade name GAVRETO ® ) was conducted in 15 healthy adult volunteers. A single 200 mg dose of pralsetinib was administer…
View article: Evaluation of Patient‐Centric Sample Collection Technologies for Pharmacokinetic Assessment of Large and Small Molecules
Evaluation of Patient‐Centric Sample Collection Technologies for Pharmacokinetic Assessment of Large and Small Molecules Open
Low‐volume sampling devices offer the promise of lower discomfort and greater convenience for patients, potentially reducing patient burden and enabling decentralized clinical trials. In this study, we determined whether low‐volume samplin…
View article: Exploring the Impact of Hepatic Impairment on Pralsetinib Pharmacokinetics
Exploring the Impact of Hepatic Impairment on Pralsetinib Pharmacokinetics Open
Pralsetinib is a kinase inhibitor indicated for the treatment of metastatic rearranged during transfection (RET) fusion-positive non-small cell lung cancer. Pralsetinib is primarily eliminated by the liver and hence hepatic impairment (HI)…
View article: Understanding <scp>CYP3A4</scp> and P‐gp mediated <scp>drug–drug</scp> interactions through <scp>PBPK</scp> modeling – Case example of pralsetinib
Understanding <span>CYP3A4</span> and P‐gp mediated <span>drug–drug</span> interactions through <span>PBPK</span> modeling – Case example of pralsetinib Open
Pralsetinib, a potent and selective inhibitor of oncogenic RET fusion and RET mutant proteins, is a substrate of the drug metabolizing enzyme CYP3A4 and a substrate of the efflux transporter P‐gp based on in vitro data. Therefore, its phar…
View article: Pharmacokinetics (PK) of Tiragolumab in First‐in‐Human Study in Patients with Mixed Solid Tumors (GO30103)
Pharmacokinetics (PK) of Tiragolumab in First‐in‐Human Study in Patients with Mixed Solid Tumors (GO30103) Open
Tiragolumab is a first‐in‐class, fully human IgG1/kappa anti‐TIGIT monoclonal antibody that blocks the binding of TIGIT to CD155 (the poliovirus receptor). We summarize the pharmacokinetics (PK) data from the phase 1a/1b GO30103 study of Q…
View article: Risk Factors of Hyperglycemia After Treatment With the AKT Inhibitor Ipatasertib in the Prostate Cancer Setting: A Machine Learning–Based Investigation
Risk Factors of Hyperglycemia After Treatment With the AKT Inhibitor Ipatasertib in the Prostate Cancer Setting: A Machine Learning–Based Investigation Open
PURPOSE Hyperglycemia is a major adverse event of phosphatidylinositol 3-kinase/AKT inhibitor class of cancer therapeutics. Machine learning (ML) methodologies can identify and highlight how explanatory variables affect hyperglycemia risk.…
View article: Safety Profile of Ipatasertib Plus Abiraterone vs Placebo Plus Abiraterone in Metastatic Castration-resistant Prostate Cancer
Safety Profile of Ipatasertib Plus Abiraterone vs Placebo Plus Abiraterone in Metastatic Castration-resistant Prostate Cancer Open
Ipatasertib plus abiraterone had an overall tolerable safety profile consistent with known toxicities. More AEs leading to drug discontinuation were observed with ipatasertib than placebo, but incidence would likely be lessened with prophy…
View article: Characterization of exposure–response relationships of ipatasertib in patients with metastatic castration-resistant prostate cancer in the IPATential150 study
Characterization of exposure–response relationships of ipatasertib in patients with metastatic castration-resistant prostate cancer in the IPATential150 study Open
Purpose The exposure–response relationships for efficacy and safety of ipatasertib, a selective AKT kinase inhibitor, were characterized using data collected from 1101 patients with metastatic castration-resistant prostate cancer in the IP…
View article: Mitigating ipatasertib‐induced glucose increase through dose and meal timing modifications
Mitigating ipatasertib‐induced glucose increase through dose and meal timing modifications Open
Ipatasertib, an AKT inhibitor, in combination with prednisone and abiraterone, is under evaluation for the treatment of metastatic castration‐resistant prostate cancer (mCRPC). Hyperglycemia is an on‐target effect of ipatasertib. An open‐l…
View article: Drug–Drug Interaction Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Ipatasertib in Combination with Darolutamide in Patients with Advanced Prostate Cancer
Drug–Drug Interaction Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Ipatasertib in Combination with Darolutamide in Patients with Advanced Prostate Cancer Open
Ipatasertib is a selective, small molecule Akt inhibitor that is currently being developed for the treatment of metastatic castration-resistant prostate cancer. Darolutamide is an androgen receptor (AR) inhibitor that is approved for the t…
View article: Pharmacokinetics of Ipatasertib in Subjects With Hepatic Impairment Using 2 Methods of Classification of Hepatic Function
Pharmacokinetics of Ipatasertib in Subjects With Hepatic Impairment Using 2 Methods of Classification of Hepatic Function Open
Ipatasertib is a highly selective small‐molecule pan‐Akt inhibitor in clinical development. Ipatasertib is predominantly eliminated by the liver, and therefore, the effect of hepatic impairment on ipatasertib pharmacokinetics (PK) was eval…
View article: Evaluation of Ipatasertib Interactions with Itraconazole and Coproporphyrin I and III in a Single Drug Interaction Study in Healthy Subjects
Evaluation of Ipatasertib Interactions with Itraconazole and Coproporphyrin I and III in a Single Drug Interaction Study in Healthy Subjects Open
Ipatasertib is a pan-AKT inhibitor in development for the treatment of cancer. Ipatasertib was metabolized by CYP3A4 to its major metabolite, M1 (G-037720), and was a P-gp substrate and OATP1B1/1B3 inhibitor in vitro. A phase I drug-drug i…
View article: Calibrating the In Vitro–In Vivo Correlation for OATP-Mediated Drug-Drug Interactions with Rosuvastatin Using Static and PBPK Models
Calibrating the In Vitro–In Vivo Correlation for OATP-Mediated Drug-Drug Interactions with Rosuvastatin Using Static and PBPK Models Open
Organic anion-transporting polypeptide (OATP) 1B1/3-mediated drug-drug interaction (DDI) potential is evaluated in vivo with rosuvastatin (RST) as a probe substrate in clinical studies. We calibrated our assay with RST and estradiol 17-β-D…
View article: Acute hemiballismus in the absence of subthalamic nucleus lesion
Acute hemiballismus in the absence of subthalamic nucleus lesion Open
A 68-year-old male, known hypertensive on irregular medication presented with sudden onset of involuntary movements of the left upper limb, in the form of severely violent, arrhythmic, and flinging large amplitude movements for 2 days, sug…
View article: Quantitative Prediction of OATP‐Mediated Drug‐Drug Interactions With Model‐Based Analysis of Endogenous Biomarker Kinetics
Quantitative Prediction of OATP‐Mediated Drug‐Drug Interactions With Model‐Based Analysis of Endogenous Biomarker Kinetics Open
Quantitative prediction of the magnitude of transporter‐mediated clinical drug‐drug interactions (DDIs) solely from in vitro inhibition data remains challenging. The objective of the present work was to analyze the kinetic profile of an en…