Raltegravir

Raltegravir is an HIV-1 antiviral drug [see Microbiology (12.4) ] .

• ISENTRESS® is indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV-1) infection in patients 4 weeks of age and older. The use of other active agents with ISENTRESS is associated with a greater likelihood of treatment response [see Clinical Studies (14) ] .ICD-10: B20

• None None ( 4 ).contraindicated

ISENTRESS can be administered with or without food ( 2.1 ). Do not substitute ISENTRESS chewable tablets or ISENTRESS for oral suspension for the ISENTRESS 400 mg film-coated tablet. See specific dosing guidance for chewable tablets and the formulation for oral suspension ( 2.1 ). Adults 400 mg film-coated tablet orally, twice daily ( 2.2 ). During coadministration with rifampin in adults, 800 mg twice daily ( 2.1 ). Children and Adolescents If at least 25 kg: One 400 mg film-coated tablet orally, twice daily. If unable to swallow a tablet, consider the chewable tablet, as specified in Table 1 ( 2.3 ). If at least 3 kg to less than 25 kg: Weight based dosing, as specified in Table 2. For patients weighing between 11 and 20 kg, either the chewable tablet or the formulation for oral suspension can be used, as specified in Table 2 ( 2.3 ). 2.1 General Dosing Recommendations ISENTRESS Film-Coated Tablets, Chewable Tablets and For Oral Suspension can be administered with or without food [see Clinical Pharmacology (12.3) ] . Because the formulations are not bioequivalent, do not substitute ISENTRESS chewable tablets or ISENTRESS for oral suspension for the ISENTRESS 400 mg film-coated tablet. See specific dosing guidance for chewable tablets and the formulation for oral suspension. During coadministration of ISENTRESS 400 mg film-coated tablets with rifampin, the recommended dosage of ISENTRESS is 800 mg twice daily in adults. There are no data to guide co-administration of ISENTRESS with rifampin in patients below 18 years of age [see Drug Interactions (7.2) ] .

Severe, potentially life-threatening and fatal skin reactions have been reported. This includes cases of Stevens-Johnson syndrome, hypersensitivity reaction and toxic epidermal necrolysis. Immediately discontinue treatment with ISENTRESS and other suspect agents if severe hypersensitivity, severe rash, or rash with systemic symptoms or liver aminotransferase elevations develops and monitor clinical status, including liver aminotransferases closely ( 5.1 ). Monitor for Immune Reconstitution Syndrome ( 5.2 ). Inform patients with phenylketonuria that the 100 mg and 25 mg chewable tablets contain phenylalanine ( 5.3 ). 5.1 Severe Skin and Hypersensitivity Reactions Severe, potentially life-threatening, and fatal skin reactions have been reported. These include cases of Stevens-Johnson syndrome and toxic epidermal necrolysis. Hypersensitivity reactions have also been reported and were characterized by rash, constitutional findings, and sometimes, organ dysfunction, including hepatic failure. Discontinue ISENTRESS and other suspect agents immediately if signs or symptoms of severe skin reactions or hypersensitivity reactions develop (including, but not limited to, severe rash or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema). Clinical status including liver aminotransferases should be monitored and appropriate therapy initiated.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The most common adverse reactions of moderate to severe intensity (≥2%) are insomnia, headache, dizziness, nausea and fatigue ( 6.1 ). Creatine kinase elevations were observed in subjects who received ISENTRESS. Myopathy and rhabdomyolysis have been reported. Use with caution in patients at increased risk of myopathy or rhabdomyolysis, such as patients receiving concomitant medications known to cause these conditions and patients with a history of rhabdomyolysis, myopathy or increased serum creatine kinase ( 6.2 ). To report SUSPECTED ADVERSE REACTIONS, contact Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., at 1-877-888-4231 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Treatment-Naïve Adults The following safety assessment of ISENTRESS in treatment-naïve subjects is based on the randomized double-blind active controlled study of treatment-naïve subjects, STARTMRK (Protocol 021) with ISENTRESS 400 mg twice daily in combination with a fixed dose of emtricitabine 200 mg (+) tenofovir 300 mg, (N=281) versus efavirenz (EFV) 600 mg at bedtime in combination with emtricitabine (+) tenofovir, (N=282).

Pregnancy: ISENTRESS should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus ( 8.1 ). Nursing Mothers: Breastfeeding is not recommended while taking ISENTRESS ( 8.3 ). 8.1 Pregnancy Pregnancy Category C ISENTRESS should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. There are no adequate and well-controlled studies in pregnant women. In addition, there have been no pharmacokinetic studies conducted in pregnant patients. Developmental toxicity studies were performed in rabbits (at oral doses up to 1000 mg/kg/day) and rats (at oral doses up to 600 mg/kg/day). The reproductive toxicity study in rats was performed with pre-, peri-, and postnatal evaluation. The highest doses in these studies produced systemic exposures in these species approximately 3- to 4-fold the exposure at the recommended human dose. In both rabbits and rats, no treatment-related effects on embryonic/fetal survival or fetal weights were observed. In addition, no treatment-related external, visceral, or skeletal changes were observed in rabbits. However, treatment-related increases over controls in the incidence of supernumerary ribs were seen in rats at 600 mg/kg/day (exposures 3-fold the exposure at the recommended human dose). Placenta transfer of drug was demonstrated in both rats and rabbits.

Metabolism

Adults Absorption Raltegravir (film-coated tablet) is absorbed with a T max of approximately 3 hours postdose in the fasted state. Raltegravir AUC and C max increase dose proportionally over the dose range 100 mg to 1600 mg.

No specific information is available on the treatment of overdosage with ISENTRESS. Doses as high as 1600-mg single dose and 800-mg twice-daily multiple doses were studied in healthy volunteers without evidence of toxicity. Occasional doses of up to 1800 mg per day were taken in the clinical studies of HIV-1 infected subjects without evidence of toxicity. In the event of an overdose, it is reasonable to employ the standard supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required. The extent to which ISENTRESS may be dialyzable is unknown.

• Oct 12, 2007NDANDA022145Msd Sub Merck
• Dec 21, 2011NDANDA203045Msd Sub Merck
• Dec 20, 2013NDANDA205786Msd Sub Merck

1. 1Drug Interaction1,2077.4%
2. 2Foetal Exposure During Pregnancy1,0766.6%
3. 3Depression1,0166.2%
4. 4Anxiety9665.9%
5. 5Pain9175.6%
6. 6Emotional Distress7894.8%
7. 7Exposure During Pregnancy7334.5%
8. 8Maternal Exposure During Pregnancy7324.5%
9. 9Anhedonia7084.3%
10. 10Virologic Failure5823.6%
11. 11Renal Failure5583.4%
12. 12Chronic Kidney Disease5473.3%
13. 13Fatigue5303.2%
14. 14Diarrhoea5253.2%
15. 15Nausea4692.9%

Recent PubMed references pinned to Raltegravir as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Raltegravir Plasma Exposure: A Machine Learning-Based Model for its Prediction Using Limited Sampling Strategy.
  The AAPS journal · 2026 · De Lucca Thomaz M, de Azevedo KLR, Paz TA, et al.
  PMID 42091773DOI 10.1208/s12248-026-01248-5
• Antiretroviral raltegravir, a selective human immunodeficiency virus type 1 integrase inhibitor, shows anti-Alzheimer's potential against amyloid-beta(1-42)-induced neurodegeneration.
  Mechanisms of ageing and development · 2026 · Alami M, Berrougui H, Boumezough K, et al.
  PMID 41707918DOI 10.1016/j.mad.2026.112161
• Efficacy of raltegravir in achieving virological suppression at delivery in HIV-positive pregnant women: a systematic review and meta-analysis.
  BMC pregnancy and childbirth · 2025 · Zhang Y, Wu W, Yang M, et al.
  PMID 41299398DOI 10.1186/s12884-025-08135-5
• Association of HLA-B*53 With DRESS Syndrome in Patients Treated With Raltegravir: Two Case Reports and a Literature Review.
  Basic & clinical pharmacology & toxicology · 2025 · Ramos-Del Moral C, Rodríguez Cortés P, Navares-Gómez M, et al.
  PMID 41025677DOI 10.1111/bcpt.70118
• Mapping the Gut Microbiota Composition in the Context of Raltegravir, Dolutegravir, and Bictegravir-A Scoping Review.
  International journal of molecular sciences · 2025 · Gáspár Z, Lakatos B
  PMID 40650144DOI 10.3390/ijms26136366
• Influence of concurrent oral calcium carbonate supplementation on steady-state pharmacokinetics of once daily oral raltegravir in persons with HIV: a protocol for a prospective open-label non-randomised study in Canada.
  BMJ open · 2025 · Teixeira Nunes Porto LL, Doyle MA, Zhang G, et al.
  PMID 40617620DOI 10.1136/bmjopen-2024-094384
• Analysis of raltegravir analogs to enhance inhibitory efficiency against HIV integrase.
  Scientific reports · 2025 · Sabaghian H, Yoosefian M
  PMID 40360594DOI 10.1038/s41598-025-01666-z
• Outcomes After Prenatal Exposure to Raltegravir-Containing Antiretroviral Therapy: A Multicohort European Study.
  Journal of acquired immune deficiency syndromes (1999) · 2025 · Sconza R, Fernandes G, Bailey H, et al.
  PMID 39994844DOI 10.1097/QAI.0000000000003645

The 10 most recently updated of 332 ClinicalTrials.gov registrations naming Raltegravir as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Provide Continued Access to Study Drug to Children and Adolescents Who Have Completed Clinical Studies Involving Gilead HIV Treatments
  Recruiting · Phase 4 · Interventional · 350 enrolled · Gilead Sciences
  NCT06337032updated 2026-06-10
• Reducing Antiretroviral Treatments
  Terminated · Phase 3 · Interventional · 360 enrolled · ANRS, Emerging Infectious Diseases
  NCT04051970updated 2026-06-08
• Study to Compare an Oral Weekly Islatravir/Lenacapavir Regimen With Standard of Care in Virologically Suppressed People With HIV-1
  Active not recruiting · Phase 3 · Interventional · 600 enrolled · Gilead Sciences
  NCT06630299updated 2026-05-29
• Very Early Intensive Treatment of Infants Living With HIV to Achieve HIV Remission
  Recruiting · Phase 1 · Phase 2 · Interventional · 1,120 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT02140255updated 2026-05-26
• Study of Cobicistat-Boosted Atazanavir (ATV/co), Cobicistat-Boosted Darunavir (DRV/co) and Emtricitabine/Tenofovir Alafenamide (F/TAF) in Children With HIV
  Active not recruiting · Phase 2 · Phase 3 · Interventional · 133 enrolled · Gilead Sciences
  NCT02016924updated 2026-04-21
• Renal Transplantation and Raltegravir in HIV-Infected Patients
  Completed · Phase 3 · Interventional · 27 enrolled · ANRS, Emerging Infectious Diseases
  NCT01453192updated 2026-04-13
• Antiretroviral Treatment Taken 4 Days Per Week Versus Continuous Therapy 7/7 Days Per Week in HIV-1 Infected Patients
  Completed · Phase 3 · Interventional · 640 enrolled · ANRS, Emerging Infectious Diseases
  NCT03256422updated 2026-04-13
• Kuwa Free! - Live Free!
  Recruiting · Interventional · 700 enrolled · University of Alabama at Birmingham
  NCT05044962updated 2026-04-13
• Efficacy and Tolerance of the Switch From Enfuvirtine to Raltegravir in Antiretroviral Therapy Regimen in HIV Patients With Undetectable Viral Load
  Completed · Phase 3 · Interventional · 170 enrolled · French National Agency for Research on AIDS and Viral Hepatitis
  NCT00454337updated 2026-04-06
• Raltegravir in Patients With End Stage Liver Disease and in Transplant Recipients
  Completed · Phase 1 · Phase 2 · Interventional · 14 enrolled · ANRS, Emerging Infectious Diseases
  NCT01022476updated 2026-04-06

CPIC-curated drug–gene pairs for Raltegravir. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• UGT1A1CPIC B/C (provisional)FDA label: No Clinical PGx

Frequently asked questions

How does Raltegravir work?

Raltegravir is an HIV-1 antiviral drug [see Microbiology (12.4) ] .

What is Raltegravir used for?

According to FDA labeling, Raltegravir carries indications including: ISENTRESS® is indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV-1) infection in patients 4 weeks of age and older. The use of other active agents with ISENTRESS is associated with a greater likelihood of treatment response [see Clinical Studies (14) ] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Raltegravir?

Raltegravir is classified as Integrase inhibitors, Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor, HIV Integrase Inhibitors, Decreased DNA Integrity.

What are the brand names for Raltegravir?

Raltegravir is marketed under brand names including Isentress.

What are the contraindications for Raltegravir?

Raltegravir labeling lists contraindications including: None None ( 4 ).. Always consult the full prescribing information and a clinician.