Induction of CYP3A4 by efavirenz in primary human hepatocytes: comparison with rifampin and phenobarbital

N Hariparsad, SC Nallani, RS Sane… - The Journal of …, 2004 - Wiley Online Library
The antiretroviral agent efavirenz enhances the systemic clearance of coadministered drugs
that are cytochrome P450 (CYP) 3A4 substrates. The mechanism of the apparent increase …

Induction of cytochrome P450 3A4 in primary human hepatocytes and activation of the human pregnane X receptor by tamoxifen and 4-hydroxytamoxifen

PB Desai, SC Nallani, RS Sane, LB Moore… - Drug metabolism and …, 2002 - ASPET
Tamoxifen is a widely utilized antiestrogen in the treatment and chemoprevention of breast
cancer. Clinical studies document that tamoxifen administration markedly enhances the …

Digoxin is not a substrate for organic anion-transporting polypeptide transporters OATP1A2, OATP1B1, OATP1B3, and OATP2B1 but is a substrate for a sodium …

ME Taub, K Mease, RS Sane, CA Watson… - Drug metabolism and …, 2011 - ASPET
Digoxin, an orally administered cardiac glycoside cardiovascular drug, has a narrow
therapeutic window. Circulating digoxin levels (maximal concentration of ∼1.5 ng/ml) require …

Evaluation of ipatasertib interactions with itraconazole and coproporphyrin I and III in a single drug interaction study in healthy subjects

RS Sane, KWK Cheung, E Cho, BM Liederer… - … of Pharmacology and …, 2021 - ASPET
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 …

Mechanisms underlying benign and reversible unconjugated hyperbilirubinemia observed with faldaprevir administration in hepatitis C virus patients

RS Sane, GG Steinmann, Q Huang, Y Li, L Podila… - … of Pharmacology and …, 2014 - ASPET
Faldaprevir, an investigational agent for hepatitis C virus treatment, is well tolerated but
associated with rapidly reversible, dose-dependent, clinically benign, unconjugated …

Defining the role of gut bacteria in the metabolism of deleobuvir: in vitro and in vivo studies

M McCabe, RS Sane, M Keith-Luzzi, J Xu, I King… - Drug Metabolism and …, 2015 - ASPET
Deleobuvir is a potent inhibitor of the hepatitis C virus nonstructural protein 5B polymerase.
In humans, deleobuvir underwent extensive reduction to form CD 6168. This metabolite was …

Contribution of major metabolites toward complex drug-drug interactions of deleobuvir: in vitro predictions and in vivo outcomes

RS Sane, D Ramsden, JP Sabo, C Cooper… - Drug Metabolism and …, 2016 - ASPET
The drug-drug interaction (DDI) potential of deleobuvir, an hepatitis C virus (HCV) polymerase
inhibitor, and its two major metabolites, CD 6168 (formed via reduction by gut bacteria) …

Mitigating ipatasertib‐induced glucose increase through dose and meal timing modifications

…, H Hinton, JD Gallo, G Rasuo, RS Sane - Clinical and …, 2022 - Wiley Online Library
Ipatasertib, an AKT inhibitor, in combination with prednisone and abiraterone, is under
evaluation for the treatment of metastatic castration‐resistant prostate cancer (mCRPC). …

Role of human pregnane X receptor in tamoxifen-and 4-hydroxytamoxifen-mediated CYP3A4 induction in primary human hepatocytes and LS174T cells

RS Sane, DJ Buckley, AR Buckley, SC Nallani… - Drug metabolism and …, 2008 - ASPET
Previously we observed that the antiestrogens tamoxifen and 4-hydroxytamoxifen (4OHT)
induce CYP3A4 in primary human hepatocytes and activate human pregnane X receptor (PXR…

Mass Balance, Metabolite Profile, and In Vitro-In Vivo Comparison of Clearance Pathways of Deleobuvir, a Hepatitis C Virus Polymerase Inhibitor

…, D Ramsden, DA Mandarino, RS Sane - Antimicrobial Agents …, 2015 - Am Soc Microbiol
The pharmacokinetics, mass balance, and metabolism of deleobuvir, a hepatitis C virus (HCV)
polymerase inhibitor, were assessed in healthy subjects following a single oral dose of …