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Strategic Considerations In HIV Therapy 

Changes in HIV Clinical Epidemiology with Therapy 

• Certain opportunistic diseases essentially disappeared

- CMV, MAC rare. KS uncommon and

• Some conditions relatively unchanged

- NHL, community acquired pneumonia

HIV Science: Open Issues

• The degree and quality of immune repair following ARV therapy

• Mechanisms of HIV pathogenesis: Is HIV non-cytopathic?

• HIV reservoirs and eradication

• Early events in HIV infection: The "real" receptor and HIV, antiretroviral, protease inhibitors, AIDS, protase

How Long Does Treatment Benefit on Immune System Persist?

  • Uncertain

- CD4 rises in vast majority of aggressively treated patients

- Rise as good with incomplete viral response

- CD4 count stable for 18+ months even after plasma virus becomes detectable

• Implications for considering treatment changes significant. If very prolonged, may wait longer to

 

CDC Spectrum of Disease Study

• Prospectively following 44,672 patients at 100 sites. Medical record audits

• ARV therapy decreases mortality

- One drug by 62%, two by 76%, three by 85% • Greater fall in MAC in gay men than IDU

• Risk of PCP directly related to CD4# and an increase to a "safe" level following ARV therapy as protective as in untreated

 

Controversies in HIV Treatment

• When is it best to start treatment

• More options for initial therapy

• Increasing complexity of treatment monitoring. What is success? - Ultrasensitive RNA assays Resistance testing

The Ideal Time to Treat HIV

• Before any significant risk for serious complications

• Before immune system is irreversibly damaged at a clinically significant level

• Before HIV evolves to more virulent form

• Before disease progression to point that compromises therapy response

• When patient is fully committed to regimen

 

The Problem of Eradication

• May be various types of latently infected cells in reservoir

• 1/10,000 CD4 Ro+ cells have integrated latent HIV

- Total population about 1 M, larger number cells in blood have inducible HIV but non-integrated

- Reservoir of comparable size in acute infection

• Estimate 23-27 years to eliminate pool but may be less if replication is an important source of replenishing pool

 

Usual Choices for Initial Therapy

• Two nucleoside RT inhibitors and one protease inhibitor

- Variation is to use two PIs to increase either potency or convenience

• Two nucleoside RT inhibitors and one non-nucleoside RT inhibitor

• Less proven options:

- Above with hydroxyurea, nnRTI+PI, three RTIs

 

Options for Initial Therapy

How to Monitor HIV Therapy

• Baseline CD4, plasma viral load

• Plasma viral load after 4 weeks

- Want to see at least 0.5 log reduction

• Plasma viral load after 8 weeks

- Want <500 copies to predict 75% probability of suppression below 50 copies at 24 weeks

• CD4 cell counts with any plasma viral load

- Want >250 cells by 3 weeks

 

Ultrasensitive HIV RNA Assays

• More sensitive limits (20-200 copies/mL) monitors more aggressive therapy

• Evidence that suppression below this level is important

- Limits resistance evolution

- Prolongs duration of suppression

• Adds some complexity to therapy

- Longer time to reach treatment goal

- Intermittent detection

- Uncertainty of clinical utility

(80% below 500 copies also below 50 copies)

 

Dangers in HIV Therapy

• Treatment may allow selection of chug resistant viruses

- May result in disease progression

- May lead to community multidrug resistance if transmitted

• Treatment may have toxicities after long-term use

 

Transmission of Drug-Resistant HIV

• Hecht et al reported on case of acute infection with multiple resistant HIV

- Virus shared resistant genotype with source (heavily treated patient with high viral load)

- Resistant genotype and phenotype to RT and protease drugs

- Slower response to conventional aggressive therapy

• Similar reports from Swiss study

 

Long-Term Protease Toxicities

• Lipodystrophies (84%, severe in 12%)

• Glucose intolerance/diabetes mellitus (23%)

• Hyperlipidemias (90%)

• Cutaneous reactions (dry skin, ingrown mils)

Proportions are those of Cart et al. Many groups report lower rates.

A New Contender for Initial Therapy?

The Role of the Non-Nucleoside Reverse-Transcriptase Inhibitors (NNRTIs)

• Three drugs in the United States

- Nevirapine, delavirdine, efavirenz

- Chemical structure, dosing, toxicity, effect on cytochrome p450 differs. All cross resistance and high level resistance can happen quickly

- Potency high in vitro. Never directly compared in vivo but general belief that EFV>NVP>DLV

- Use in initial therapy increasing even before Geneva given concerns, re: PI toxicities

 

Efavirenz Triple Therapy Results

% <400 copies at 24 wks (% <40)

On treatment LOCF N=F

Arm A = ZDV + 3TC + El~g0 (76) 88 (62) 74

Arm B = EFV + IND 90 (64) 72 ($0) 65

Arm C -- ZDV + 3TC + INId0 (72) 65 (48) 55

On treatment only uses available data (least stringent). LOCF assumes last known value (RNA, CD4), continues into future. N=F assumes treatment failure after data is missing (most stringent), CD4 rise of 140 cells in each group

Triple Therapy With No Protease or nnRTI

• Fischl et t al reported on a trial of ZDV+3?C+ the new RTI, abacavir

• 173 patients, no prior therapy, randomized to ZDV+3TC vs ZDV+$TC+ABC

• At 16 weeks, 75%<400 (54%<50) with three drugs vs only 35% <400 with two drugs

• Advantage is simplicity; 6 tabs da/ly total in a BID regimen that can be taken with food

• ABC hypersensitivity in about 3% (early)

 

Hydroxyurea

• No independent HIV activity

• Increases effective intracellular level of nucleosides (especially ddI) by reducing concentration of competing substrate

• In ACTG 307, significantly increased antiviral potency of ddI but blocked CD4 increase

• No known resistance and may restore ddl sensitivity

• Toxicity includes neutropenia, alopecia

"Compacting" HIV Treatment

• Realize that adherence can be improved with easier regimens; fewer pills, less frequent dosing, less dietary restriction

• BID regimens increasingly of interest:

- ZDV, 3TC, d4T, ddl, nevirapine, efavirenz, ritonavir all BID (or QD, for some)

- Preliminary BID data promising with nelfinavir, indinavir, saquinavir-sgc

When Has Treatment Failed?

• Possibilities

- Plasma viral load above detection limits

- Viral load becomes detectable after initial response

- CD4 count falls or fails to rise

- Resistance tests show sentinel mutations in patient with stable viral load

- Patient experiences toxicity or clinical progression

Applying Resistance Testing in Clinical Management

• Baseline testing in acute HIV infection

• Community monitoring of resistance prevalence to recommend best initial therapy

• Testing at time of virologic failure to select drugs to discontinue

• Testing at time of therapy change to select best regimen

New Life for the Salk Vaccine?

• Valentine et al treated 43 patients with PI regimen with or without killed vaccine (RernuneTM) at 4, 16, 28 wks

• Both groups had similar RNA, CD4 effects at wk 20

• RemuneTM group had better immune parameters including HIV antigen response. This crossed HIV clades.