Pipeline Research

Islatravir: evaluation of clinical development for HIV and HBV

Islatravir, Pipeline Research / By

Islatravir (ISL) is a nucleoside reverse transcriptase translocation inhibitor (NRTTI) that disrupts HIV reverse transcriptase through multiple mechanisms and retains a 3’OH group, unlike other approved NtRTIs. The drug has demonstrated high potency and tolerability in both in vitro and clinical studies. The review covers the historical development of ISL, its mechanisms of action against […]

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Modeling of HIV-1 prophylactic efficacy and toxicity with islatravir shows non-superiority for oral dosing, but promise as a subcutaneous implant

Islatravir, Pipeline Research / By

HIV prevention with pre-exposure prophylaxis (PrEP) is crucial, but daily oral adherence can be challenging. Long-acting (LA) PrEP formulations, such as islatravir (ISL), offer a solution with less frequent dosing. A mathematical model using phase II trial data found that ISL implants at 56–62 mg effectively reduce HIV risk without adversely affecting lymphocyte counts, whereas

Modeling of HIV-1 prophylactic efficacy and toxicity with islatravir shows non-superiority for oral dosing, but promise as a subcutaneous implant Read More »

Antiviral potency of long-acting islatravir subdermal implant in SHIV-infected macaques

Islatravir, Pipeline Research / By

Treatment nonadherence in people living with HIV  poses significant risks, including drug resistance, disease progression, and increased morbidity and mortality. Long-acting antiretroviral therapies, such as islatravir (ISL), offer a potential solution by minimizing the need for frequent dosing. This study demonstrates that a subdermal long-acting nanofluidic implant delivering ISL effectively reduces viral load in SHIV-infected

Antiviral potency of long-acting islatravir subdermal implant in SHIV-infected macaques Read More »

Current status of the small molecule anti-HIV drugs in the pipeline or recently approved

Apretude, Islatravir, Pipeline Research / By

HIV/AIDs presents significant treatment challenges due to increasing resistance to current antiretroviral drugs. This resistance is exacerbated in low- and middle-income countries due to drug misuse, inadequate drug supply, and poor treatment monitoring. Despite these challenges, there has been progress in developing new ARV drugs targeting various components of HIV. This review, updated as of

Current status of the small molecule anti-HIV drugs in the pipeline or recently approved Read More »

Physiologically Based Pharmacokinetic Modelling of Cabotegravir Microarray Patches in Rats and Humans

Pipeline Research / By

Microarray patches (MAPs) are currently under investigation as a self-administered, pain-free alternative used to achieve long-acting (LA) drug delivery. Cabotegravir is a potent antiretroviral with superior results over current pre-exposure prophylaxis (PrEP) regimens. This study aimed to apply physiologically based pharmacokinetic (PBPK) modeling to describe the pharmacokinetics of the dissolving bilayer MAP platform and predict

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Efficacy and safety of oral islatravir once daily in combination with doravirine through 96 weeks for treatment-naïve adults with HIV-1 infection receiving initial treatment with islatravir, doravirine, and lamivudine

Islatravir / By

Conclusion: ISL/DOR-based regimens maintained viral suppression through week 96. ISL/DOR regimens were well tolerated regardless of dose.

Efficacy and safety of oral islatravir once daily in combination with doravirine through 96 weeks for treatment-naïve adults with HIV-1 infection receiving initial treatment with islatravir, doravirine, and lamivudine Read More »

Islatravir Has a High Barrier to Resistance and Exhibits a Differentiated Resistance Profile from Approved Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Islatravir / By

While A114S conferred reduced susceptibility to ISL, it increased susceptibility to approved nucleoside reverse transcriptase inhibitors (NRTIs). This differential impact of A114S on ISL, an NRTTI, compared to NRTIs likely results from the different mechanisms of action. Altogether, the results demonstrate that ISL has a high barrier to resistance and a differentiated mechanism compared to

Islatravir Has a High Barrier to Resistance and Exhibits a Differentiated Resistance Profile from Approved Nucleoside Reverse Transcriptase Inhibitors (NRTIs) Read More »

Development and validation of ion-pairing HPLC-CAD chromatography for measurement of Islatravir’s phosphorylated intermediates

Islatravir / By

While the Islatravir biocatalytic cascade is an efficient and green synthetic route, the production of three non-isolated intermediates presented an analytical challenge. A robust and quantitative ion-pairing HPLC-CAD method was successfully developed and validated for use across all key intermediates within the biocatalytic cascade, providing a streamlined approach to in-process monitoring and quantification of intermediates

Development and validation of ion-pairing HPLC-CAD chromatography for measurement of Islatravir’s phosphorylated intermediates Read More »

Doravirine and Islatravir Have Complementary Resistance Profiles and Create a Combination with a High Barrier to Resistance

Islatravir / By

In de novo resistance selection studies in MT4-GFP cells (MT4 cells engineered to express green fluorescent protein), DOR/ISL synergistically prevented viral breakthrough at a threshold of 2× the half-maximal inhibitory concentration (IC50). DOR/ISL exhibited a higher barrier to resistance than DOR/3TC and dolutegravir (DTG)/3TC. Resistance analysis showed no emergence of substitutions at F227, an observation

Doravirine and Islatravir Have Complementary Resistance Profiles and Create a Combination with a High Barrier to Resistance Read More »

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