New England Journal of Medicine December 30, 2010

Preexposure Chemoprophylaxis for HIV Prevention in Men Who Have Sex with Men

Robert M. Grant, Javier R. Lama, Peter L. Anderson, et al.

Bottom Line

The iPrEx trial demonstrated that a daily oral combination of emtricitabine and tenofovir disoproxil fumarate (FTC-TDF) significantly reduces the risk of HIV acquisition in high-risk men and transgender women who have sex with men, with efficacy strongly dependent on medication adherence.

Key Findings

1. In the modified intention-to-treat analysis, there were 36 incident HIV infections in the FTC-TDF group compared to 64 in the placebo group, representing a 44% relative reduction in HIV incidence (95% CI, 15 to 63; P=0.005).
2. Efficacy was highly correlated with medication adherence; participants with detectable study drug levels in their blood experienced a 92% relative reduction in the risk of HIV acquisition (95% CI, 40 to 99; P<0.001) compared to those without detectable drug.
3. Among those assigned to FTC-TDF, the study drug was detected in 51% of seronegative subjects but only 9% of those who became HIV-infected.
4. By self-reported adherence, visits where participants reported taking the drug 90% or more of the days were associated with a 73% reduction in HIV acquisition risk (95% CI, 41 to 88).
5. Safety profiles were similar between the two groups with no significant differences in serious adverse events (P=0.57), though mild nausea was more frequently reported in the FTC-TDF arm during the first 4 weeks (P<0.001).
6. No new emtricitabine or tenofovir resistance mutations were observed among the 100 participants who became infected during the follow-up period; however, among the 10 individuals who were unknowingly HIV-positive at baseline, 2 developed emtricitabine resistance.

Study Design

Design
Randomized Controlled Trial
Double-Blind
Sample
2,499
Patients
Duration
1.2 yr
Median
Setting
Multinational
Population HIV-seronegative men and transgender women who have sex with men (MSM) at high risk for HIV acquisition.
Intervention Daily oral combination of emtricitabine and tenofovir disoproxil fumarate (FTC-TDF).
Comparator Matching daily oral placebo.
Outcome Incident HIV infection.

Study Limitations

Overall intention-to-treat efficacy (44%) was heavily attenuated by suboptimal adherence, underscoring a major real-world vulnerability of daily oral prophylaxis regimens.
Only 29 participants (approximately 1%) identified as transgender women, limiting the study's statistical power to definitively evaluate efficacy within this highly vulnerable subpopulation.
Intensive clinical trial conditions, which included monthly visits, pill counts, extensive risk-reduction counseling, and frequent STI testing, may be difficult to replicate and scale in resource-limited, real-world settings.
The study specifically enrolled men and transgender women who have sex with men, meaning the efficacy results could not immediately be generalized to heterosexual couples or people who inject drugs (though later trials confirmed PrEP efficacy in these groups).

Clinical Significance

The iPrEx trial was a landmark study that revolutionized modern HIV prevention by providing the first definitive clinical evidence for the efficacy of pre-exposure prophylaxis (PrEP). Its findings directly led to the 2012 FDA approval of Truvada for HIV prevention, ushering in an era of biomedical prophylaxis that shifted the global paradigm beyond solely behavioral interventions (e.g., condoms). By demonstrating a stark contrast between an overall 44% risk reduction and a 92% reduction among participants with detectable drug levels, the trial established medication adherence as the absolute critical determinant of PrEP success—a principle that has guided all subsequent clinical implementation and catalyzed the development of long-acting prevention modalities.

Historical Context

Prior to 2010, the global response to the HIV epidemic relied almost exclusively on behavioral modifications, condom distribution, testing, and treating known infected individuals to reduce transmission (treatment as prevention). Biomedical prevention strategies for uninfected individuals, such as topical microbicides and HIV vaccines, had historically yielded disappointing or merely modest results (e.g., the RV144 vaccine trial). The concept of giving daily systemic antiretroviral therapy to uninfected, high-risk individuals to prevent viral establishment was theoretically sound but lacked definitive human data. The iPrEx trial was launched in 2007 across 6 countries to test this hypothesis in MSM, a population disproportionately affected by the epidemic.

Guided Discussion

High-yield insights from every perspective

Med Student
Medical Student

What is the mechanism of action of emtricitabine (FTC) and tenofovir disoproxil fumarate (TDF), and why are two agents used together for pre-exposure prophylaxis rather than a single agent?

Key Response

FTC and TDF are both nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) that competitively inhibit viral reverse transcriptase and cause chain termination. Using two agents provides a higher barrier to resistance and synergistic antiviral activity compared to monotherapy, crucial for preventing establishment of infection if exposure occurs.

Resident
Resident

When initiating a patient on FTC-TDF for PrEP based on the iPrEx trial, what baseline testing and ongoing clinical monitoring are essential to ensure patient safety and prevent medication-associated complications?

Key Response

Baseline and quarterly HIV testing are critical to avoid PrEP use during unrecognized acute HIV, which can lead to resistant strains. Additionally, baseline renal function and HBV serology must be assessed, as TDF can cause nephrotoxicity and its discontinuation can precipitate severe acute exacerbation of hepatitis B.

Fellow
Fellow

The iPrEx trial showed a strong correlation between detectable drug levels and HIV protection. How does the pharmacokinetic profile of TDF/FTC differ in rectal versus vaginal tissues, and how does this impact adherence counseling for MSM compared to heterosexual women?

Key Response

TDF/FTC concentrates much faster and achieves higher, more stable active diphosphate levels in rectal tissue compared to cervicovaginal tissue. Consequently, PrEP provides robust protection for receptive anal intercourse with fewer doses per week (estimated 4 doses/week), whereas near-perfect daily adherence is required for optimal protection during receptive vaginal intercourse.

Attending
Attending

Given the high efficacy of PrEP in highly adherent patients, risk compensation (increased unprotected sex) was a major concern prior to the iPrEx trial. How did the trial findings address this concern, and how should this influence how we frame PrEP discussions with hesitant colleagues?

Key Response

The iPrEx trial actually showed a decrease in self-reported unprotected receptive anal intercourse and an increase in condom use over time in both study arms. This suggests that engaging in a PrEP program, which includes regular counseling and STI testing, does not necessarily lead to risk compensation and may actually reinforce overall safe sexual practices, a key teaching point for providers hesitant to prescribe it.

Scholarly Review

Critical appraisal through the lens of expert reviewers and guideline development

PhD
PhD

In the iPrEx trial, adherence was measured via self-report, pill counts, and drug-level testing in a subset of participants. How does the discrepancy between self-reported adherence and objective pharmacokinetic data highlight the limitations of traditional adherence measures in prevention trials, and what novel trial designs could mitigate this bias?

Key Response

Self-reported adherence in iPrEx was nearly perfectly high, yet drug-level testing revealed that only a fraction of those who acquired HIV had detectable drug levels. This demonstrates significant social desirability bias. Future trials could utilize objective biomarkers (e.g., intra-erythrocytic drug levels) as primary covariates in adherence-efficacy models or employ directly observed long-acting formulations to eliminate the daily adherence variable entirely.

Journal Editor
Journal Editor

The iPrEx trial utilized an intent-to-treat (ITT) analysis to demonstrate a 44% overall reduction in HIV incidence, but the reduction was much higher (92%) in the subgroup with detectable drug levels. As a reviewer, what are the epidemiological hazards of highlighting the 92% efficacy figure in the abstract or conclusions?

Key Response

Highlighting the 92% efficacy derived from the subset with detectable drug levels constitutes a per-protocol or as-treated analysis, which breaks the randomization and introduces confounding (e.g., highly adherent patients might also engage in lower-risk behaviors). As an editor, one must ensure the primary ITT results (44% reduction) remain the focal point to accurately reflect real-world population-level effectiveness and avoid overstating the drug's practical impact.

Guideline Committee
Guideline Committee

The iPrEx trial provided the foundational evidence for CDC and WHO guidelines recommending daily oral FTC-TDF for PrEP in MSM. How should guideline committees weigh the advent of on-demand (2-1-1) PrEP dosing and long-acting injectables (like cabotegravir) against the established iPrEx daily oral paradigm?

Key Response

While iPrEx established daily FTC-TDF as a Category 1A recommendation, subsequent trials (like IPERGAY for 2-1-1 dosing and HPTN 083 for long-acting cabotegravir) offer alternatives that address the adherence challenges highlighted in iPrEx. Guidelines must now stratify PrEP recommendations based on patient preference, adherence capacity, and sexual practices, maintaining daily FTC-TDF as a standard while upgrading alternatives to high-strength recommendations to maximize population coverage.

Clinical Landscape

Noteworthy Related Trials

2012

Partners PrEP Trial

n = 4747 · NEJM

Tested

Daily oral TDF or TDF-FTC

Population

Heterosexual HIV serodiscordant couples

Comparator

Placebo

Endpoint

HIV infection

Key result: Daily TDF and TDF-FTC reduced the risk of HIV acquisition by 67 percent and 75 percent, respectively.
2015

PROUD Trial

n = 544 · Lancet

Tested

Daily oral TDF-FTC

Population

MSM at high risk for HIV

Comparator

Deferred PrEP

Endpoint

HIV infection

Key result: Early initiation of daily PrEP reduced HIV incidence by 86 percent compared with deferred initiation.
2015

IPERGAY Trial

n = 400 · NEJM

Tested

Event-driven (on-demand) oral TDF-FTC

Population

High-risk MSM

Comparator

Placebo

Endpoint

HIV infection

Key result: On-demand PrEP taken before and after sexual activity reduced the risk of HIV infection by 86 percent.

Tailored to your role

Want this tailored to you?

Add your specialty or training stage to get role-specific takeaways and more questions.

Personalize this analysis