Injectable Antiretroviral Drugs: Back to the Future

Berruti, Marco; Riccardi, Niccolò; Canetti, Diana; Caputo, Sergio Lo; Taramasso, Lucia; Biagio, Antonio Di

doi:10.3390/v13020228

Cited by 9 publications

(8 citation statements)

References 37 publications

(41 reference statements)

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“…In recent years, parenteral and long-acting (LA) formulations have been studied [16]. Indeed, LAs will contribute to achieving the treatment goals of ART: maximal and durable suppression of plasma viremia delays and prevention of the selection of drug-resistant mutations, preservation or improvement of CD4 T lymphocyte (CD4) cell numbers, and the conference of substantial clinical benefits.…”

Section: Introductionmentioning

confidence: 99%

Could Long-Acting Cabotegravir-Rilpivirine Be the Future for All People Living with HIV? Response Based on Genotype Resistance Test from a Multicenter Italian Cohort

Vito

Botta

Berruti

et al. 2022

JPM

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Long-acting (LA) formulations have been designed to improve the quality of life of people with HIV (PWH) by maintaining virologic suppression. However, clinical trials have shown that patient selection is crucial. In fact, the HIV-1 resistance genotype test and the Body Mass Index of individual patients assume a predominant role in guiding the choice. Our work aimed to estimate the patients eligible for the new LA therapy with cabotegravir (CAB) + rilpivirine (RPV). We selected, from the Antiviral Response Cohort Analysis (ARCA) database, all PWH who had at least one follow-up in the last 24 months. We excluded patients with HBsAg positivity, evidence of non-nucleoside reverse transcriptase inhibitor (except K103N) and integrase inhibitor mutations, and with a detectable HIV-RNA (>50 copies/mL). Overall, 4103 patients are currently on follow-up in the ARCA, but the eligible patients totaled 1641 (39.9%). Among them, 1163 (70.9%) were males and 1399 were Caucasian (85.3%), of which 1291 (92%) were Italian born. The median length of HIV infection was 10.2 years (IQR 6.3–16.3) with a median nadir of CD4 cells/count of 238 (106–366) cells/mm3 and a median last available CD4 cells/count of 706 (509–944) cells/mm3. The majority of PWH were treated with a three-drug regimen (n = 1116, 68%). Among the 525 (30.3%) patients treated with two-drug regimens, 325 (18.1%) were treated with lamivudine (3TC) and dolutegravir (DTG) and only 84 (5.1%) with RPV and DTG. In conclusion, according to our snapshot, roughly 39.9% of virologically suppressed patients may be suitable candidates for long-acting CAB+RPV therapy. Therefore, based on our findings, many different variables should be taken into consideration to tailor the antiretroviral treatment according to different individual characteristics.

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Section: Introductionmentioning

confidence: 99%

Could Long-Acting Cabotegravir-Rilpivirine Be the Future for All People Living with HIV? Response Based on Genotype Resistance Test from a Multicenter Italian Cohort

Vito

Botta

Berruti

et al. 2022

JPM

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“…In the present study, the completion rate of all subjects for preventive oral drugs was 64.0%, and drug adherence was observed to be 75.7%, indicating that a large proportion of subjects were unable to consume oral drugs on a regular basis, or discontinued the medication. ABT is a long-acting injectable drug approved for antiretroviral use in China [ 25 ]. In our study, ABT was administered on the 1st and 15th days.…”

Section: Discussionmentioning

confidence: 99%

Tolerability and Adherence of Antiretroviral Regimens Containing Long-Acting Fusion Inhibitor Albuvirtide for HIV Post-Exposure Prophylaxis: A Cohort Study in China

Nie

Sun

et al. 2021

Infect Dis Ther

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Introduction: There have been no prospective clinical studies investigating adherence and tolerability of HIV post-exposure prophylaxis (PEP) in China. Tolerability, adherence, and transmitted drug resistance are concerns, especially when single-tablet regimen (STR) usage is low. The present study aimed to explore the safety, tolerability, and adherence of regimens containing albuvirtide (ABT) compared with recommended non-STR antiretrovirals for HIV PEP. Methods: This was a prospective, open-label, multicenter cohort study. The subjects were stratified into 3 groups based on their preference: ABT ? Dolutegravir (DTG) (Group 1), ABT ? Tenofovir disoproxil fumarate (TDF) ? Lamivudine (3TC) (Group 2), and DTG ? TDF ? 3TC (Group 3). All enrolled subjects received PEP within 72 h after exposure and continued for 28 days, and were followedup for 12 weeks. Results: A total of 330 participants were enrolled in the three groups. Most participants were male (87.2%). Sexual contact was the most frequent mode of exposure (91.9%). The average time from exposure to treatment was 26.8 ± 19.5 h. There were no statistically significant differences between the three study groups with respect to completion of oral medication at 28 days. The 28-day completion rate was shown to be significantly higher with ABT versus oral (88.9% vs. 64.0%; p\0.0001), and adherence with ABT was 94.4% compared to 75.7% with oral PEP (p\0.0001). Subjects in ABT-containing Group 1 exhibited higher adherence than those in Group 3 (87.3% vs. 72.9%; p\0.05). None of the participants reported serious adverse drug reactions which led to withdrawal from the study. All the drug regimens were found to be safe and well tolerated. No HIV incident case was observed during the study period.Conclusions: ABT-containing regimens (ABT ? DTG or ABT ? TDF ? 3TC) offer a good option for HIV PEP due to higher completion rates and adherence than the DTG ? TDF ? 3TC regimen. The overall safety was comparable and acceptable among the three groups.Jingmin Nie and Feng Sun have contributed equally to this work.

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“…Lopinavir (53), for example, was developed as a PK enhancer to act in combination with Ritonavir (49) to improve the potency. The combination at different ratios exhibits promising in vitro inhibition against CYP3A (IC 50 = 1.1, 4.6 μM) compared to other PIs.…”

Section: Second-generation Pismentioning

confidence: 99%

“…ENF, the first peptide-based HIV FI, was approved by the U.S. FDA in 2003 for clinical application in the treatment of HIV/AIDS patients who have shown resistance to existing ARV medications. 49 It is a lipopeptide drug with a sequence similar to the HR-2, a heptad repeat domain in the region of the gp41 protein (Figure 3). By competitively blocking the HR-2 component of gp41 from attaching to HR-1, it prevents gp41 from binding to another trimeric heptad domain.…”

Section: Fusion Inhibitorsmentioning

confidence: 99%

Pharmacological advances in anti‐retroviral therapy for human immunodeficiency virus‐1 infection: A comprehensive review

Azzman,

Gill,

Hassan

et al. 2024

Reviews in Medical Virology

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The discovery of anti‐retroviral (ARV) drugs over the past 36 years has introduced various classes, including nucleoside/nucleotide reverse transcriptase inhibitors, non‐nucleoside reverse transcriptase inhibitors, protease inhibitor, fusion, and integrase strand transfer inhibitors inhibitors. The introduction of combined highly active anti‐retroviral therapies in 1996 was later proven to combat further ARV drug resistance along with enhancing human immunodeficiency virus (HIV) suppression. As though the development of ARV therapies was continuously expanding, the variation of action caused by ARV drugs, along with its current updates, was not comprehensively discussed, particularly for HIV‐1 infection. Thus, a range of HIV‐1 ARV medications is covered in this review, including new developments in ARV therapy based on the drug's mechanism of action, the challenges related to HIV‐1, and the need for combination therapy. Optimistically, this article will consolidate the overall updates of HIV‐1 ARV treatments and conclude the significance of HIV‐1‐related pharmacotherapy research to combat the global threat of HIV infection.

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Injectable Antiretroviral Drugs: Back to the Future

Cited by 9 publications

References 37 publications

Could Long-Acting Cabotegravir-Rilpivirine Be the Future for All People Living with HIV? Response Based on Genotype Resistance Test from a Multicenter Italian Cohort

Could Long-Acting Cabotegravir-Rilpivirine Be the Future for All People Living with HIV? Response Based on Genotype Resistance Test from a Multicenter Italian Cohort

Tolerability and Adherence of Antiretroviral Regimens Containing Long-Acting Fusion Inhibitor Albuvirtide for HIV Post-Exposure Prophylaxis: A Cohort Study in China

Pharmacological advances in anti‐retroviral therapy for human immunodeficiency virus‐1 infection: A comprehensive review

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