Atazanavir

Atazanavir is an HIV-1 antiretroviral drug [see Microbiology (12.4) ] .

• REYATAZ ® is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and in pediatric patients 3 months and older weighing at least 5 kg. Limitations of Use: • REYATAZ is not recommended for use in pediatric patients below the age of 3 months due to the risk of kernicterus [see Use in Specific Populations (8.4) ] .ICD-10: B20

• REYATAZ is contraindicated: • in patients with previously demonstrated clinically significant hypersensitivity (eg, Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions) to any of the components of REYATAZ capsules or REYATAZ oral powder [see Warnings and Precautions (5.2) ] . • when coadministered with drugs that are highly dependent on CYP3A or UGT1A1 for clearance, and for which elevated plasma concentrations of the interacting drugs are associated with serious and/or life-threatening events (see Table 6).contraindicated

• Pretreatment testing: Renal laboratory testing should be performed in all patients prior to initiation of REYATAZ and continued during treatment with REYATAZ. Hepatic testing should be performed in patients with underlying liver disease prior to initiation of REYATAZ and continued during treatment with REYATAZ. (2.2) • Treatment-naive adults: REYATAZ 300 mg with ritonavir 100 mg once daily with food or REYATAZ 400 mg once daily with food. (2.3) • Treatment-experienced adults: REYATAZ 300 mg with ritonavir 100 mg once daily with food. (2.3) • Pediatric patients: REYATAZ capsule dosage is based on body weight not to exceed the adult dose and must be taken with food. (2.4) • REYATAZ oral powder: Must be taken with ritonavir and food and should not be used in pediatric patients who weigh less than 5 kg. (2.5) • Pregnancy: REYATAZ 300 mg with ritonavir 100 mg once daily with food, with dosing modifications for some concomitant medications. (2.6) • Dosing modifications: may be required for concomitant therapy ( 2.3 , 2.4 , 2.5 , 2.6) , renal impairment (2.7) , and hepatic impairment. (2.8) 2.1 Overview • REYATAZ capsules and oral powder must be taken with food. • Do not open the capsules. • The recommended oral dosage of REYATAZ depends on the treatment history of the patient and the use of other coadministered drugs. When coadministered with H 2 -receptor antagonists or proton-pump inhibitors, dose separation may be required [see Dosage and Administration (2.3 , 2.4 , 2.5 , and 2.6 ) and Drug Interactions (7) ] .

• Cardiac conduction abnormalities: PR interval prolongation may occur in some patients. ECG monitoring should be considered in patients with preexisting conduction system disease or when administered with other drugs that may prolong the PR interval. (5.1 , 7.3 , 12.2 , 17) • Severe Skin Reactions: Discontinue if severe rash develops. (5.2 , 17) • Hyperbilirubinemia: Most patients experience asymptomatic increases in indirect bilirubin, which is reversible upon discontinuation. Do not dose reduce. If a concomitant transaminase increase occurs, evaluate for alternative etiologies. (5.8) • Phenylketonuria: REYATAZ oral powder contains phenylalanine which can be harmful to patients with phenylketonuria. (5.3) • Hepatotoxicity: Patients with hepatitis B or C virus are at risk of increased transaminases or hepatic decompensation. Monitor hepatic laboratory tests prior to therapy and during treatment. (2.8 , 5.4 , 8.8) • Chronic kidney disease has been reported during postmarketing surveillance in patients with HIV-1 treated with atazanavir, with or without ritonavir. Consider alternatives in patients at high risk for renal disease or with preexisting renal disease. Monitor renal laboratory tests prior to therapy and during treatment. Consider discontinuation of REYATAZ in patients with progressive renal disease. (5.5) • Nephrolithiasis and cholelithiasis have been reported. Consider temporary interruption or discontinuation. (5.6) • The concomitant use of REYATAZ with ritonavir and certain other medications may result in known or potentially significant drug interactions.

The following adverse reactions are discussed in greater detail in other sections of the labeling: • cardiac conduction abnormalities [see Warnings and Precautions (5.1) ] • rash [see Warnings and Precautions (5.2) ] • hyperbilirubinemia [see Warnings and Precautions (5.8) ] • chronic kidney disease [see Warnings and Precautions (5.5) ] • nephrolithiasis and cholelithiasis [see Warnings and Precautions (5.6) ] Most common adverse reactions (≥2%) are nausea, jaundice/scleral icterus, rash, headache, abdominal pain, vomiting, insomnia, peripheral neurologic symptoms, dizziness, myalgia, diarrhea, depression, and fever. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Bristol-Myers Squibb at 1-800-721-5072 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trial Experience 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. Adverse Reactions in Treatment-Naive Adult Participants The safety profile of REYATAZ in treatment-naive adults is based on 1625 participants with HIV-1 in clinical trials. 536 participants received REYATAZ 300 mg with ritonavir 100 mg and 1089 participants received REYATAZ 400 mg or higher (without ritonavir). The most common adverse reactions were nausea, jaundice/scleral icterus, and rash.

• Pregnancy: Available human and animal data suggest that atazanavir does not increase the risk of major birth defects overall compared to the background rate. (8.1) • Hepatitis B or C co-infection: Monitor liver enzymes. (5.4 , 6.1) • Renal impairment: REYATAZ is not recommended for use in treatment-experienced patients with end-stage renal disease managed with hemodialysis. (2.7 , 8.7) • Hepatic impairment: REYATAZ is not recommended in patients with severe hepatic impairment. REYATAZ with ritonavir is not recommended in patients with any degree of hepatic impairment. (2.8 , 8.8) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in patients exposed to REYATAZ during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Atazanavir has been evaluated in a limited number of women during pregnancy. Available human and animal data suggest that atazanavir does not increase the risk of major birth defects overall compared to the background rate [see Data ] . In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Metabolism

The pharmacokinetics of atazanavir were evaluated in adult participants who either were healthy, or with HIV-1, after administration of REYATAZ 400 mg once daily and after administration of REYATAZ 300 mg with ritonavir 100 mg once daily (see Table 17). Table 17: Steady-State Pharmacokinetics of Atazanavir in Healthy Participants or Participants with HIV-1 in the Fed State a n=26.

Human experience of acute overdose with REYATAZ is limited. Single doses up to 1200 mg (three times the 400 mg maximum recommended dose) have been taken by healthy participants without symptomatic untoward effects. A single self-administered overdose of 29.2 g of REYATAZ in a patient with HIV-1 (73 times the 400-mg recommended dose) was associated with asymptomatic bifascicular block and PR interval prolongation. These events resolved spontaneously. At REYATAZ doses resulting in high atazanavir exposures, jaundice due to indirect (unconjugated) hyperbilirubinemia (without associated liver function test changes) or PR interval prolongation may be observed [see Warnings and Precautions (5.1 , 5.8) and Clinical Pharmacology (12.2) ] . Treatment of overdosage with REYATAZ should consist of general supportive measures, including monitoring of vital signs and ECG, and observations of the patient’s clinical status. If indicated, elimination of unabsorbed atazanavir should be achieved by emesis or gastric lavage. Administration of activated charcoal may also be used to aid removal of unabsorbed drug. There is no specific antidote for overdose with REYATAZ.

• Jun 20, 2003NDANDA021567Bristol Myers Squibb
• Apr 22, 2014ANDAANDA091673Teva Pharms Usa
• Jun 2, 2014NDANDA206352Bristol Myers Squibb
• Jan 29, 2015NDANDA206353Bristol
• Jun 25, 2018ANDAANDA204806Aurobindo Pharma
• Apr 30, 2021ANDAANDA212579Laurus
• Feb 2, 2022ANDAANDA212278Hetero Labs Ltd Iii

1. 1Drug Interaction1,79212%
2. 2Depression1,3179.1%
3. 3Foetal Exposure During Pregnancy1,0487.3%
4. 4Anxiety8786.1%
5. 5Maternal Exposure During Pregnancy7555.2%
6. 6Pain7555.2%
7. 7Emotional Distress6604.6%
8. 8Anhedonia6014.2%
9. 9Abortion Spontaneous5213.6%
10. 10Renal Failure4793.3%
11. 11Nephrolithiasis4733.3%
12. 12Nausea4723.3%
13. 13Fatigue4172.9%
14. 14Chronic Kidney Disease4072.8%
15. 15Osteoporosis4032.8%

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

• [Study of the possibility of isolating atazanavir from biological fluids for the purpose of chemical-toxicological analysis].
  Sudebno-meditsinskaia ekspertiza · 2026 · Illarionova EA, Zherbakova VA, Chmelevskaya NV, et al.
  PMID 41995241DOI 10.17116/sudmed20266902132
• Prevalence and correlates of hyperbilirubinemia among people living with HIV (PLHIV) receiving atazanavir boosted with ritonavir (ATV/r).
  BMC gastroenterology · 2025 · Farrokhi H, Shahmohamadi E, Pashaei A, et al.
  PMID 41291449DOI 10.1186/s12876-025-04489-4
• Coadministration of a crystalline drug compromises supersaturation and membrane transport of an amorphous drug.
  International journal of pharmaceutics · 2026 · Alkalla N, Alhalaweh A, Bergström CAS, et al.
  PMID 41241164DOI 10.1016/j.ijpharm.2025.126388
• Population pharmacokinetics of ritonavir as a booster of lopinavir, atazanavir, or darunavir in African children with HIV.
  Antimicrobial agents and chemotherapy · 2025 · Tsirizani L, Waalewijn H, Szubert A, et al.
  PMID 41004270DOI 10.1128/aac.00771-25
• Optimizing amorphous multidrug formulations: A particle engineering approach through spray drying.
  European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2025 · El Sayed M, Alhalaweh A, Asdagh A, et al.
  PMID 40983141DOI 10.1016/j.ejps.2025.107285
• Model-based evaluation of the interaction between ritonavir-boosted atazanavir and rifampicin in Ugandan adults with HIV.
  British journal of clinical pharmacology · 2025 · Kengo A, Resendiz-Galvan JE, Najjemba L, et al.
  PMID 40796001DOI 10.1002/bcp.70195
• Nanotechnology-Driven Strategy Against SARS-CoV-2: Pluronic F127-Based Nanomicelles with or Without Atazanavir Reduce Viral Replication in Calu-3 Cells.
  Viruses · 2025 · Ricci-Junior E, Rosa AS, do Nascimento T, et al.
  PMID 40284961DOI 10.3390/v17040518
• Intracellular Penetration of Atazanavir, Ritonavir and Dolutegravir With Concomitant Rifampicin: A Dose Escalation Study.
  Clinical pharmacology and therapeutics · 2025 · De Nicolò A, Palermiti A, Mugerwa H, et al.
  PMID 39891354DOI 10.1002/cpt.3572

The 10 most recently updated of 250 ClinicalTrials.gov registrations naming Atazanavir 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
• 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
• 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
• Early and Intermittent Antiretroviral Therapy in Naive HIV Infected Adults
  Completed · Phase 2 · Interventional · 45 enrolled · ANRS, Emerging Infectious Diseases
  NCT00820118updated 2026-04-07
• Measure of Pharmacokinetic Parameters and Adherence With MEMS in Naive HIV Infected Patients Treated With Reyataz Once Daily Combined With Norvir and Truvada
  Completed · Phase 2 · Interventional · 35 enrolled · French National Agency for Research on AIDS and Viral Hepatitis
  NCT00528060updated 2026-04-06
• Population Pharmacokinetics of Antiretroviral in Children
  Completed · Observational · 65 enrolled · Assistance Publique - Hôpitaux de Paris
  NCT03194165updated 2026-04-03
• Dual Boosted Protease Inhibitor Regimens Without Any Additional Antiretroviral Therapy in HIV-1 Infected Patients (ANRS127)
  Completed · Phase 2 · Interventional · 61 enrolled · French National Agency for Research on AIDS and Viral Hepatitis
  NCT00122603updated 2026-04-02
• Telaprevir in HIV-HCV Coinfected Patients Who Had Previously Failed a Peginterferon-Ribavirin Regimen
  Completed · Phase 2 · Interventional · 70 enrolled · ANRS, Emerging Infectious Diseases
  NCT01332955updated 2026-04-02
• Study Evaluating the Efficacy, Safety, and Tolerability of Switching to Long-acting Cabotegravir Plus Long-acting Rilpivirine From Current Antiretroviral Regimen in Virologically Suppressed HIV-1-infected Adults
  Active not recruiting · Phase 3 · Interventional · 618 enrolled · ViiV Healthcare
  NCT02951052updated 2025-12-31

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

• UGT1A1CPIC AClinPGx 1A
  UGT1A1 and Atazanavir

Frequently asked questions

How does Atazanavir work?

Atazanavir is an HIV-1 antiretroviral drug [see Microbiology (12.4) ] .

What is Atazanavir used for?

According to FDA labeling, Atazanavir carries indications including: REYATAZ ® is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and in pediatric patients 3 months and older weighing at least 5 kg. Limitations of Use: • REYATAZ is not recommended for use in pediatric patients below the age of 3 months due to the risk of kernicterus [see Use in Specific Populations (8.4) ] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Atazanavir?

Atazanavir is classified as Protease inhibitors, Protease Inhibitor, Cytochrome P450 2C8 Inhibitors, Cytochrome P450 3A Inducers, Cytochrome P450 3A Inhibitors, Cytochrome P450 3A4 Inhibitors, HIV Protease Inhibitors, UDP Glucuronosyltransferases Inhibitors, UGT1A1 Inhibitors, Decreased Protein Synthesis, Increased Immunologically Active Molecule Activity.

What are the brand names for Atazanavir?

Atazanavir is marketed under brand names including Evotaz, Reyataz.

What are the contraindications for Atazanavir?

Atazanavir labeling lists contraindications including: REYATAZ is contraindicated: • in patients with previously demonstrated clinically significant hypersensitivity (eg, Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions) to any of the components of REYATAZ capsules or REYATAZ oral powder [see Warnings and Precautions (5.2) ] . • when coadministered with drugs that are highly dependent on CYP3A or UGT1A1 for clearance, and for which elevated plasma concentrations of the interacting drugs are associated with serious and/or life-threatening events (see Table 6).. Always consult the full prescribing information and a clinician.