Express delivery only needs to be taken once a month, and the Phase 2 clinical results of long-acting HIV preventive therapy are positive

▎The content team editor of WuXi PharmaTech (MSD) today announced that its innovative nucleoside reverse transcriptase translocation inhibitor (NRTTI) islatravir, as a pre-exposure prophylaxis (PrEP), has achieved positive results in phase 2a clinical trials
.

After 24 weeks, monthly oral islatravir showed good safety and tolerability, and 8 weeks after receiving the last dose of treatment, the level of islatravir in the subjects’ peripheral blood mononuclear cells (PBMCs) remained high To maintain the pharmacokinetic threshold of drug efficacy
.

PrEP is an important means to reduce HIV infection.
Taking antiviral drugs before infection can effectively reduce the risk of HIV infection in high-risk groups
.

Although oral PrEP therapy has been approved by the FDA for marketing, it needs to be taken daily.
If the medication is interrupted for some reason, it may increase the risk of HIV infection
.

Therefore, long-acting PrEP therapy is the development direction of many companies
.

Islatravir is an innovative NRTTI developed by Merck.
Preclinical studies have shown that it can inhibit the function of HIV reverse transcriptase through a variety of mechanisms.
Its mechanism of action is different from the currently approved anti-HIV therapies and traditional nucleoside reverse transcriptase inhibition.
Agents (NRTIs)
.

At present, Merck has carried out a number of clinical trials to test its effect as a single-drug PrEP therapy and in combination with other antiviral therapies to treat HIV infection
.

▲Islatravir's research and development plan (picture source: reference [2]) In this randomized, double-blind, placebo-controlled phase 2a clinical trial, 242 participants with low risk of being infected by HIV were randomly divided into three groups , Once a month oral dose of 60 or 120 mg islatravir, or placebo
.

The results of the trial showed that islatravir showed good safety, and only less than 1% (n=2) of the participants withdrew from the trial due to adverse events (AE)
.

The unblinded safety data showed that most AEs were mild.
The most common AEs in the 60 mg, 120 mg, and placebo groups of islatravir were headache (10.
3%, 9.
3%, 4.
2%), diarrhea (5.
2%) , 5.
2%, 8.
3%) and nausea (5.
2%, 7.
2%, 4.
2%)
.

No serious drug-related adverse events were found in subjects taking islatravir
.

Pharmacokinetic studies have shown that the minimum concentration of islatravir in peripheral blood mononuclear cells during the treatment period is still higher than the preset threshold that can maintain the therapeutic effect
.

And it was maintained after receiving the last dose of islatravir for 8 weeks
.

Dr.
Joan Butterton, Vice President of Global Clinical Development for Infectious Diseases of Merck Laboratories, said that this result not only further accumulates the pharmacokinetic data of islatravir, but also provides encouraging features for its safety and tolerability as a PrEP therapy.
Support
.

Reference: [1] Merck Presents New Data from Ongoing Phase 2a Clinical Trial Evaluating the Safety, Tolerability and Pharmacokinetics of Investigational, Once-Monthly, Oral Islatravir for HIV-1 Prevention at IAS 2021.
Retrieved July 20, 2021, from https: // oral-islatravir-for-hiv-1-prevention-at-ias-2021/[2] slatravir Clinical Program Overview.
Retrieved July 20, 2021, from https:// /5/2021/07/ISL-Pipeline-Document-7-7-21.
pdf Note: This article aims to introduce the progress of medical and health research, not a treatment plan recommendation
.

If you need guidance on treatment plans, please go to a regular hospital for treatment
.