Tipranavir: a novel second-generation nonpeptidic protease inhibitor.

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Hi All

Below is the abstarct of the article that I published on Tipranvir- a new

Protease Inhibitor. If you would like to have the complete article contact me

(see contact info at bottom of email).

Vijayabhaskar Reddy Kandula

E-mail: <emailreddy@...>

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Tipranavir: a novel second-generation nonpeptidic protease inhibitor.

Kandula VR, Khanlou H, Farthing C.

AIDS Healthcare Foundation, 1300 N Vermont Avenue, Suite 407, Los Angeles, CA

90027, USA. reddy@...

Tipranavir is a new nonpeptidic protease inhibitor and belongs to the class of

4-hydroxy-5, 6-dihydro-2-pyrones. Chemically, tipranavir is based on coumarin

and sulfonamide compounds, amongst others. It exhibits potent and specific

activity against both HIV-1 and -2. Tipranavir 500 mg in combination with

ritonavir 200 mg twice daily results in optimum viral load reduction and

suppresses both wild-type and protease inhibitor-resistant virus. It is

metabolized by the cytochrome P4503A4 enzyme and its pharmacokinetic parameters

are enhanced when combined with ritonavir.

Tipranavir is excreted primarily in the feces, with minimal excretion in urine.

In early trials, tipranavir/ritonavir was demonstrated to be safe and well

tolerated, with mild gastrointestinal side effects.

Preliminary data indicate pharmacokinetic interaction with nucleotide reverse

transcriptase inhibitors; however, no dose adjustments are recommended at this

time. Virologic response is not adequate when combined with other

ritonavir-boosted protease inhibitors, and is currently not recommended. As with

other protease inhibitors, tipranavir interacts with fluconazole, atorvastatin,

clarithromycin and rifabutin and absorption is reduced when taken with antacids

and didanosine (enteric coated formulation). Phase III trials are underway to

compare the efficacy of tipranavir/ritonavir with other antiretroviral agents.

_________________

Vijayabhaskar Reddy Kandula MD MPH

HIV Physician

740 S St s Pl Apt 16, Los Angeles CA 90005

Ph: 213 382 8521, Cell: 626 - 215 - 0569

E-mail: <emailreddy@...>