Treatment Review No. 23 - December 1996

3TC (lamivudine, Epivir):

Approved nucleoside analog reverse transcriptase inhibitor. 3TC has also shown activity against the hepatitis B virus. Side effects can include headache, nausea, low white blood cells and rare cases of hair loss.

Abacavir (1592U89):

Experimental nucleoside analog reverse transcriptase inhibitor. Similar to AZT but has stronger anti-HIV effects. Main side effects seen so far are rash and headache. This drug may become available by prescription in late 1997.

adefovir dipivoxil (PMEA):

Experimental nucleotide analog antiviral drug. Effective against many different herpesviruses, as well as HIV. Now being studied in combination with other anti-HIV drugs. Dosing is one pill a day. This drug may become available by prescription in late 1997.

AZT (zidovudine, Retrovir):

Approved nucleoside analog reverse transcriptase inhibitor. Long-term AZT use is associated with loss of muscle. Other side effects can be nausea, vomiting, anemia, low white blood cells, bone marrow damage, and headaches. Also approved for preventing transmission of HIV from mother to child.

d4T (stavudine, Zerit):

Approved nucleoside analog reverse transcriptase inhibitor. Side effects can include nerve damage in the hands and feet (peripheral neuropathy), stomach upset, damage to the pancreas (pancreatitis) and liver damage.

ddC (zalcitabine, HIVID):

Approved nucleoside analog reverse transcriptase inhibitor. Side effects can include peripheral neuropathy, pancreatitis, and sores in the mouth.

ddI (didanosine, Videx):

Approved nucleoside analog reverse transcriptase inhibitor. Comes as chewable tablet or powder. Side effects can include peripheral neuropathy, pancreatitis, and diarrhea. ddI is coated in an antacid buffer that can effect the absorption of other drugs such as dapsone and indinavir.

delavirdine (Rescriptor):

Experimental non-nucleoside reverse transcriptase inhibitor (NNRTI). The main side effect is a rash. This drug is currently available through an expanded access program and is likely to be approved for prescription early in 1997.

DMP266:

Experimental non-nucleoside reverse transcriptase inhibitor (NNRTI). DMP-266 stays in the body for a long time and so is only taken once a day. Had strong anti-HIV effects in an early study. The drug is thought to have few side effects. If studies go well, this drug may become available by prescription in late 1997 or early in 1998.

F-ddA:

Experimental nucleoside analog reverse transcriptase inhibitor. F-ddA is related to ddI, but is expected to be better absorbed and therefore does not have to be administered with buffers. The buffers in ddI pills can make the drug difficult to take. In the test tube, F-ddA is active against HIV that is resistant to ddI. This drug is only in the first phase of human studies. fozivudine tidoxil:

Experimental nucleoside analog reverse transcriptase inhibitor, similar to AZT. This drug is only in the first phase of human studies. HBY-097:

Experimental non-nucleoside reverse transcriptase inhibitor (NNRTI). In the laboratory, HIV that is resistant to HBY-097 does not reproduce as well as normal HIV. If studies go well, this drug may become available by prescription in late 1997 or early in 1998. hydroxyurea (Hydrea):

Approved anti-cancer drug being studied for the treatment of HIV infection in combination with ddI. May help ddI work better, even if HIV has gotten resistant to the effects of ddI alone. Side effects can be nausea, vomiting and bone marrow suppression.

indinavir (Crixivan):

Approved protease inhibitor. Side effects can be nausea and kidney stones. If HIV becomes resistant to indinavir, other protease inhibitors may not work.

lobucavir:

Experimental nucleoside analog antiviral drug. Effective against many different herpesvirus types, as well as HIV. Also being studied as a CMV treatment. If studies go well, this drug may become available by prescription in late 1997 or early in 1998.

nelfinavir (AG-1343, Viracept):

Experimental protease inhibitor. The main side effect is diarrhea, which has been controlled with over the counter antidiarrheal medications when needed. This drug is currently available through an expanded access program and is expected to be approved for prescription in 1997.

nevirapine (Viramune):

Approved non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV develops resistance to this drug quickly, so it is approved for use in combination with nucleoside analog anti-HIV drugs. Not yet approved for use with protease inhibitors due to possible drug interactions. Possible side effect can be rash, which in some cases can be severe. PMPA:

Experimental nucleotide analog anti-HIV drug. May be more potent than nucleosides like AZT. Protected macaques from SIV ( a virus related to HIV) infection in animal studies. In Phase I studies in human beings.

ritonavir (Norvir):

Approved protease inhibitor. Side effects can be nausea, diarrhea and numbing around the mouth. Also effects the absorption of many other drugs by the body due to its actions in the liver. There is a long list of drugs that can not be taken when taking ritonavir.

saquinavir (Invirase):

Approved protease inhibitor. Few side effects, mainly stomach upset and gas. Not as well absorbed by the body as other protease inhibitors, which may make it easier for HIV to get resistant to saquinavir. HIV that is resistant to saquinavir may find it easier to resist the effects of other protease inhibitors. This is currently being studied in people.

VX-478 (141W94):

Experimental protease inhibitor. Well tolerated in a small 4 week Phase I study, with the main side effect being a rash. Also had a strong anti-HIV effect. Larger studies are expected to begin in early 1997.

Technical Terms

nucleoside analog:

An artificial copy of a nucleoside. Nucleosides are one of the building blocks of DNA, and DNA stores information necessary for creating any new living thing. Viruses make copies of themselves with DNA. Nucleoside analogs like AZT get into cells in the body and are mixed up with the virus' DNA as the virus tries to infect those cells. The nucleoside analog stops viral DNA from working properly. This prevents the cell from being infected, like throwing a wrench in the virus' genetic works. Nucleoside analogs may also sometimes inhibit production of human DNA in healthy cells, causing side effects. Non-nucleosides (NNRTIs) are drugs that inhibit the virus without using this mechanism.

nucleotide analog:

An artificial copy of a nucleotide. Nucleotides work in the same way as nucleosides, but they have a slightly different chemical structure. This difference in structure is thought to make it easier for these drugs to get into cells in the body to protect them from infection by HIV.

reverse transcriptase inhibitors:

Reverse transcriptase is a part of HIV required to infect cells in the body and make more virus. Drugs that inhibit reverse transcriptase stop HIV from infecting uninfected cells in the body. They do not help cells that have already been infected with the virus.

protease inhibitors:

Protease inhibitors are non-nucleoside drugs that inhibit protease, an enzyme that HIV uses when it releases new virus from an infected cell. Unlike drugs that inhibit reverse transcriptase, protease inhibitors stop cells that are already infected from making new virus.

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