May 2004
| Antiretroviral Drug | FDA Pregnancy Category* | Placental Passage (Newborn:Mother Drug Ratio) | Long-term Animal Carcino- genicity Studies |
Animal Teratogen Studies |
| Nucleoside and Nucleotide Analogue Reverse Transcriptase Inhibitors | ||||
| Abacavir (Ziagen, ABC) | C | Yes (rats) | Positive (malignant and non-malignant tumors of liver, thyroid in female rats, and preputial and clitoral gland of mice and rats) | Positive (rodent anasarca and skeletal malformations at 1,000 mg/kg (35x human exposure) during organogenesis; not seen in rabbits) |
| Didanosine (Videx, ddI) | B | Yes (human) [0.5] | Negative (no tumors, lifetime rodent study) | Negative |
| Emtricitabine (Emtriva, FTC) | B | Unknown | Not completed | Negative |
| Lamivudine (Epivir, 3TC) | C | Yes (human) [~1.0] | Negative (no tumors, lifetime rodent study) | Negative |
| Stavudine (Zerit, d4T) | C | Yes (rhesus monkey) [0.76] | Positive (mice and rats, at very high dose exposure, liver and bladder tumors) | Negative (but sternal bone calcium decreases in rodents) |
| Tenofovir DF (Viread) | B | Yes (rat and monkey) | Not completed | Negative (osteomalacia when given to juvenile animals at high doses) |
| Zalcitabine (HIVID, ddC) | C | Yes (rhesus monkey) [0.30-0.50] | Positive (rodent, thymic lymphomas) | Positive (rodent- |
| Zidovudine (Retrovir, AZT, ZDV) | C | Yes (human) [0.85] | Positive (rodent, noninvasive vaginal epithelial tumors) | Positive (rodent-near lethal dose) |
| Non-Nucleoside Reverse Transcriptase Inhibitors | ||||
| Delavirdine (Rescriptor) | C | Unknown | Positive (hepatocellular adenomas and carcinomas in male and female mice but not rats, bladder tumors in male mice) | Positive (rodent- |
| Efavirenz (Sustiva) | C | Yes (cynomologus monkey, rat, rabbit)[~1.0] | Positive (increased hepatocellular adenomas and carcinomas and pulmonary alveolar/ |
Positive (cynomo- logus monkey- |
| Nevirapine (Viramune) | C | Yes (human)[~1.0] | Positive (hepatocellular adenomas and carcinomas in mice and rats) | Negative |
| Protease Inhibitors | ||||
| Amprenavir (Agenerase) | C | Unknown | Positive (hepatocellular adenomas and carcinomas in male mice and rats) | Negative (but deficient ossification and thymic elongation in rats and rabbits) |
| Atazanavir | B | Unknown | Not Completed | Negative |
| Fosamprenavir (Lexiva) | C | Unknown | Positive (increased benign and malignant liver tumors in male rodents) | Negative (deficient ossification with amprenavir but not fosamprenavir) |
| Indinavir (Crixivan) | C | Minimal (humans) | Positive (thyroid adenomas in male rats at highest dose) | Negative (but extra ribs in rodents) |
| Lopinavir/ Ritonavir (Kaletra) |
C | Unknown | Not Completed | Negative (but delayed skeletal ossification and increase in skeletal variations in rats at maternally toxic doses) |
| Nelfinavir (Viracept) | B | Minimal (humans) | Positive (thyroid follicular adenomas and carcinomas in rats) | Negative |
| Ritonavir (Norvir) | B | Minimal (humans) | Positive (rodent, liver adenomas and carcinomas in male mice) | Negative (but cryptorchidism in rodents) |
| Saquinavir (Fortovase) | B | Minimal (humans) | Not completed | Negative |
| Fusion Inhibitors | ||||
| Enfuvirtide (Fuzeon) | B | Unknown | Not Done | Negative |
* FDA pregnancy categories:
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