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Elvucitabine
el-vue-SYE-ta-been

Other Names: ACH-126443

Drug Class: Nucleoside Reverse Transcriptase Inhibitors

Elvucitabine is a type of medicine called a nucleoside reverse transcriptase inhibitor (NRTI). NRTIs block reverse transcriptase, a protein that HIV needs to make more copies of itself.

HIV/AIDS-Related Uses

Elvucitabine is an investigational medicine that is not yet approved by the FDA for use outside of clinical trials. It is being studied for the treatment of HIV infection. Elvucitabine is similar to the FDA-approved anti-HIV drug lamivudine (Epivir). Elvucitabine may be effective in treating individuals infected with HIV strains resistant to lamivudine. Elvucitabine is also being studied for the treatment of hepatitis B virus (HBV) infection.Elvucitabine does not cure or prevent HIV infection or AIDS and does not reduce the risk of passing the virus to other people.

Dosage Form/Administration

Elvucitabine comes in pill form and is taken by mouth. Dosages that have been studied include 5 and 10 mg once daily and 20 mg once every other day.

Contraindications

Individuals should tell a doctor about any medical problems before taking this medicine.

Possible Side Effects

Along with its desired effects, elvucitabine may cause some unwanted effects. Although not all of these effects are known, serious bone marrow suppression has been reported. Bone marrow makes new blood cells; when it is suppressed, you may have lower levels of red blood cells (cells that carry oxygen to and wastes from other cells) or white blood cells (cells that fight infection). Bone marrow suppression caused by elvucitabine appears reversible; production of blood cells returns to normal once you stop taking elvucitabine. Individuals should tell a doctor if they have any of these side effects.Other side effects include mild rash, mild headache, and gastrointestinal symptoms, including upset stomach and diarrhea. Individuals should tell a doctor if these side effects continue or are bothersome.

Drug and Food Interactions

A doctor should be notified of any other medications being taken, including prescription, nonprescription (over-the-counter), or herbal medications.

Clinical Trials

Click here to search ClinicalTrials.gov for trials that use Elvucitabine.

Manufacturer Information

Elvucitabine

Achillion Pharmaceuticals
300 George Street
New Haven, CT 06511
Phone: 203-624-7000

Last Updated: April 5, 2009

Drug Description

Elvucitabine, also known as ELV, ACH-126443, L-Fd4C or beta-L-Fd4C, is an L-cytosine nucleoside analogue of stavudine with potent activity against HIV and chronic hepatitis B. [1] [2]

Dosing Information

Mode of Delivery

Oral. [1]

Dosage Form

In clinical trials, dosages studied include 5 and 10 mg once daily and 20 mg once every other day. [2] [3]

References

[1] Achillion Pharmaceuticals Pipeline: HIV Program - Elvucitabine. Available at: http://www.achillion.com/main.aspx?pn=ProductPipeline&fl=l. Accessed 04/05/09.

[2] Achillion Pharmaceuticals Pipeline: HIV Program - Elvucitabine. Available at: http://www.achillion.com/main.aspx?pn=ProductPipeline&fl=l. Accessed 04/05/09.

[3] HIV and Hepatitis.com Pharmacology of Elvucitabine Enables Innovative Dosing Regimens. Coverage of the 45th Interscience Conference on Antimicrobial Agents and Chemotherapy, December 16-19, 2005. Available at: http://www.hivandhepatitis.com/2005icr/icaac/docs/011306_a.html. Accessed 04/05/09.

Pharmacology

Elvucitabine is a beta-L-(-) nucleoside analogue developed to improve upon the antiviral activity of lamivudine, an FDA-approved beta-L-(-) nucleoside analogue. Compared with lamivudine, elvucitabine may allow for less frequent dosing and dose escalation, overcoming viral resistance. [1] Pharmacokinetic modeling suggests that elvucitabine maintains potent antiretroviral activity, even at doses low enough to avoid bone marrow toxicity. [2] [3] Elvucitabine inhibits wild-type HIV and HIV expressing the M184V mutation associated with lamivudine resistance. [4]

Elvucitabine has excellent oral bioavailability and a prolonged plasma half-life of greater than 100 hours. Early-stage clinical results suggest that elvucitabine's steady-state occurs following 21 days of dosing. [5] [6] [7]

In a 21-day study of 24 HIV-infected patients receiving elvucitabine at dosages of 5 or 10 mg once daily, or 20 mg every 48 hours with concomitant lopinavir/ritonavir (LPV/r) every 12 hours, viral load, compared to baseline, decreased 1.8, 1.9, and 2.0 log, respectively. Due to elvucitabine's extended half-life, LPV/r was continued to day 35 in the 10 and 20 mg cohorts. Concentrations of elvucitabine remained above the 50% inhibitory concentration (IC50) at Day 28, supporting weekly or twice-weekly dosing. The 20 mg every 48 hours cohort appeared most efficacious and minimized resistance and adherence concerns. [8]

Results from the 48-week treatment segment of a randomized, double-blind phase II trial of elvucitabine in combination with two additional antiretrovirals, efavirenz and tenofovir,as compared to lamivudine (3TC) in combination with the same two additional antiretrovirals, demonstrated elvucitabine antiviral potency to be similar to 3TC. In the elvucitabine-treated group, 96% of patients reached undetectable viral load, defined as achieving fewer than 50 copies/mL after 48 weeks of therapy. [9]