Last reviewed · How we verify
Retrovir (ZIDOVUDINE)
Retrovir works by mimicking the natural building blocks of DNA to prevent HIV from replicating.
Zidovudine (Retrovir), marketed by GSK, is a nucleoside reverse transcriptase inhibitor (NRTI) used for the treatment of HIV-1 infection, with a key composition patent expiring in 2028. Its mechanism of action, which mimics natural DNA building blocks to inhibit HIV replication, provides a well-established therapeutic option in the NRTI class. However, the presence of multiple off-patent competitors, including didanosine, zalcitabine, stavudine, lamivudine, and abacavir, poses a significant threat to market share and revenue.
At a glance
| Generic name | ZIDOVUDINE |
|---|---|
| Sponsor | GSK |
| Drug class | Hepatitis B Virus Nucleoside Analog Reverse Transcriptase Inhibitor [EPC] |
| Target | Thymidine kinase, cytosolic |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
| First approval | 1987 |
Mechanism of action
Zidovudine is an antiviral agent [see Clinical Pharmacology (12.4)].
Approved indications
- HIV-1 Infection Treatment
Boxed warnings
- BOXED WARNING WARNING: HEMATOLOGIC TOXICITY, MYOPATHY, LACTIC ACIDOSIS AND SEVERE HEPATOMEGALY WITH STEATOSIS, and EXACERBATIONS OF HEPATITIS B Zidovudine, a component of lamivudine and zidovudine tablets, has been associated with hematologic toxicity including neutropenia and severe anemia, particularly in patients with advanced Human Immunodeficiency Virus (HIV-1) disease [see Warnings and Precautions (5.1)]. Prolonged use of zidovudine has been associated with symptomatic myopathy [see Warnings and Precautions (5.2)]. Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues, including lamivudine and zidovudine (components of lamivudine and zidovudine tablet). Discontinue lamivudine and zidovudine tablets if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity occur [see Warnings and Precautions (5.3)]. Severe acute exacerbations of hepatitis B have been reported in patients who are co-infected with hepatitis B virus (HBV) and HIV-1 and have discontinued lamivudine, which is one component of lamivudine and zidovudine tablets. Hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in patients who discontinue lamivudine and zidovudine tablet and are co-infected with HIV-1 and HBV. If appropriate, initiation of anti-hepatitis B therapy may be warranted [see Warnings and Precautions (5.4)]. WARNING: HEMATOLOGIC TOXICITY, MYOPATHY, LACTIC ACIDOSIS AND SEVERE HEPATOMEGALY WITH STEATOSIS, and EXACERBATIONS OF HEPATITIS B See full prescribing information for complete boxed warning. • Hematologic toxicity, including neutropenia and anemia, has been associated with the use of zidovudine, a component of lamivudine and zidovudine tablets. (5.1) • Symptomatic myopathy associated with prolonged use of zidovudine. (5.2) • Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues including lamivudine and zidovudine (components of lamivudine and zidovudine tablets). Suspend treatment if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity occur. (5.3) • Severe acute exacerbations of hepatitis B have been reported in patients who are co-infected with hepatitis B virus (HBV) and human immunodeficiency virus (HIV-1) and have discontinued lamivudine, a component of lamivudine and zidovudine tablet. Monitor hepatic function closely in these patients and, if appropriate, initiate anti-hepatitis B treatment. (5.4)
Common side effects
- Headache
- Malaise & fatigue
- Fever or chills
- Diarrhea
- Nausea & vomiting
- Anorexia and/or decreased appetite
- Abdominal pain
- Abdominal cramps
- Dyspepsia
- Neuropathy
- Insomnia & other sleep disorders
- Dizziness
Drug interactions
- Stavudine
- Doxorubicine
- Nucleoside analogues (e.g., ribavirin)
- Ganciclovir
- Interferon alfa
- Ribavirin
- Other bone marrow suppressive or cytotoxic agents
- Sorbitol
Key clinical trials
- Allogeneic Hematopoietic Cell Transplantation for Peripheral T Cell Lymphoma (PHASE2)
- Virotherapy and Natural History Study of KHSV-Associated Multricentric Castleman s Disease With Correlates of Disease Activity (PHASE2)
- Study of Cobicistat-Boosted Atazanavir (ATV/co), Cobicistat-Boosted Darunavir (DRV/co) and Emtricitabine/Tenofovir Alafenamide (F/TAF) in Children With HIV (PHASE2,PHASE3)
- A Study to Provide Continued Access to Study Drug to Children and Adolescents Who Have Completed Clinical Studies Involving Gilead HIV Treatments (PHASE4)
- Natural History Study of the KSHV Inflammatory Cytokine Syndrome (KICS) (PHASE2)
- Belinostat Therapy With Zidovudine for Adult T-Cell Leukemia-Lymphoma (PHASE2)
- Effectiveness of Zidovudine vs. Zidovudine Plus Alpha Interferon vs. Interferon for Treatment of HIV
- Early Infant HIV Treatment in Botswana (PHASE2,PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Retrovir CI brief — competitive landscape report
- Retrovir updates RSS · CI watch RSS
- GSK portfolio CI