BACKGROUND Amprenavir (APV), fosamprenavir (FPV), lopinavir (LPV), ritonavir (RTV) and efavirenz (EFV) are to varying degrees substrates, inducers and inhibitors of CYP3A4. Coadministration of these drugs might result in complex pharmacokinetic drug-drug interactions. METHODS Two prospective, open-label, non-randomized studies evaluated APV and LPV steady-state pharmacokinetics in HIV-infecte...

Breast cancer resistance protein (BCRP) is a recently discovered ATP-binding cassette drug transporter. Hence, the full spectrum of therapeutic agents that interact with BCRP remains to be elucidated. Because human immunodeficiency virus protease inhibitors (HPIs) are well known P-glycoprotein (P-gp) substrates, and there is an overlap in substrate specificity between P-gp and BCRP, this study ...

Protease inhibitors (PIs) effectively inhibit replication of the human immunodeficiency virus (HIV), and reduce mortality and prolong survival in patients with HIV infection. Newer PIs saquinavir (soft gelatin capsule) and amprenavir, as well as other PIs, may be effective when administered twice/day. Adverse reactions may occur, as well as metabolic complications and interactions between PIs a...

In tumor cells with mutations in epidermal growth factor receptor (SQ20B), H-Ras (T24), or K-Ras (MIAPACA2 and A549), the inhibition of Akt phosphorylation increases radiation sensitivity in clonogenic assays, suggesting that Akt is a potential molecular target when combined with therapeutic radiation. Insulin resistance and diabetes are recognized side effects of HIV protease inhibitors (HPIs)...

N-benzoyl-N'-phenylthiourea (BFTU) compound is similar to amprenavir derivatives in the urea compound, chloroquine -NH group, and benzene ring, which a potent antiviral. This study evaluated effect of lipophilic, electronic, steric parameters BFTU on antiviral activity Covid-19. In silico docking using Autodock 4.2 confirm pkCSM webserver predict bioavailability toxicity. The SARS-CoV-2 recepto...

STUDY OBJECTIVE To evaluate the pharmacokinetic compatibility of a ritonavir-boosted indinavir-fosamprenavir combination among patients with human immunodeficiency virus (HIV). DESIGN Single-center, nonrandomized, prospective, multiple-dose, two-phase pharmacokinetic study. SETTING University research center. PATIENTS Eight adult patients with HIV infection who had been receiving and tole...

A computational study has been performed on a series of 55 compounds having (S)-N-(3-(N-(cyclopen-tylmethyl) substituted-phenylsulfonamido)-2-hydroxypropyl) acetamide backbone as HIV-1 protease inhibitors. Various combinations of these specific inhibitors fragments were formed by breaking them at central alicyclic single bonds, while retaining the core. Standard Topomer 3D models were automatic...