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Recommendations for Use of Antiretroviral Drugs in Pregnant HIV-1-Infected Women for Maternal Health and Interventions to Reduce Perinatal HIV Transmission in the United States

Appendix B: Supplement: Safety and Toxicity of Individual Antiretroviral Agents in Pregnancy

Integrase Inhibitors

Glossary of Terms for Supplement

Carcinogenic: Producing or tending to produce cancer

  • Some agents, such as certain chemicals or forms of radiation, are both mutagenic and clastogenic.
  • Genetic mutations and/or chromosomal damage can contribute to cancer formation.

Clastogenic: Causing disruption of or breakages in chromosomes

Genotoxic: Damaging to genetic material such as DNA and chromosomes

Mutagenic: Inducing or capable of inducing genetic mutation

Teratogenic: Interfering with fetal development and resulting in birth defects

Three drugs have been approved in this new class of antiretroviral (ARV) drugs aimed at inhibiting integrase, the viral enzyme that catalyzes the two-step process of insertion of HIV DNA into the genome of the human cell. Integrase catalyzes a preparatory step that excises two nucleotides from one strand at both ends of the HIV DNA and a final “strand transfer” step that inserts the viral DNA into the exposed regions of cellular DNA. The integrase inhibitor drug class targets this second step in the integration process. Integration is required for the stable maintenance of the viral genome as well as for efficient viral gene expression and replication. Integrase also affects retrotranscription and viral assembly. Host cells lack the integrase enzyme. Because HIV integrase represents a distinct therapeutic target, integrase inhibitors would be expected to maintain activity against HIV that is resistant to other classes of ARV drugs.

Dolutegravir (Tivicay, DTG)
Elvitegravir
Raltegravir (Isentress)

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