Darunavir

證據等級: L5 預測適應症: 4

目錄

  1. Darunavir
  2. Darunavir: From HIV-1 Infection to Simian Immunodeficiency Virus (SIV) Infection
    1. One-Sentence Summary
    2. Quick Overview
    3. Why is This Prediction Reasonable?
    4. Clinical Trial Evidence
    5. Literature Evidence
    6. Norway Market Information
    7. Safety Considerations
    8. Other TxGNN-Predicted Candidates (Reviewed, Not Recommended)
    9. Conclusion and Next Steps
    10. Disclaimer

## 藥師評估報告

Darunavir: From HIV-1 Infection to Simian Immunodeficiency Virus (SIV) Infection

One-Sentence Summary

Darunavir is a boosted HIV-1 protease inhibitor used as part of combination antiretroviral therapy (cART) for HIV/AIDS. The TxGNN model predicts it may be effective for Simian Immunodeficiency Virus (SIV) Infection — the primate-model correlate of HIV — but currently only 4 preclinical animal-model publications support this direction, none of which specifically test darunavir alone, and no clinical trials exist for this indication.

Quick Overview

Item Content
Original Indication Not specified in evidence pack (drug is not marketed in Norway); known pharmacological classification is HIV-1 infection, treated as part of boosted cART regimens
Predicted New Indication Simian Immunodeficiency Virus Infection
TxGNN Prediction Score 99.97%
Evidence Level L4
Norway Market Status ✗ Not Marketed
Number of Authorizations 0
Recommended Decision Hold

Why is This Prediction Reasonable?

Currently, detailed mechanism of action data is not available. Based on known information, darunavir is a member of the HIV-1 protease inhibitor (PI) class, its efficacy in HIV-1 infection (as part of boosted cART) has been proven, and mechanistically it may be applicable to SIV infection.

SIV is the retrovirus used to establish AIDS models in non-human primates and is genetically and structurally closely related to HIV-1, including a substantial degree of conservation in the Gag-Pol polyprotein processing pathway that PI-class drugs target. This cross-species mechanistic similarity is a well-established rationale for using HIV antiretrovirals, including PIs, in SIV-infected macaque research models.

However, it is important to note that the four supporting publications describe multi-drug cART regimens (some combined with adjunct agents such as the HDAC inhibitor SAHA or the gold compound auranofin) used in SIV/macaque reservoir and eradication research — darunavir (or PI-class drugs generally) appears only as one backbone component, not as the specific subject of efficacy testing. No study isolates or quantifies darunavir's individual contribution to SIV suppression.

Clinical Trial Evidence

Currently no related clinical trials registered.

Literature Evidence

PMID Year Type Journal Key Findings
26150024 2016 Animal Cohort AIDS Res Hum Retroviruses Compared two novel injectable coformulated cART regimens (PI-class backbone) for suppressing SIV replication in rhesus macaques
25033210 2014 Animal Cohort PLoS One Evaluated suppressive cART plus HDAC inhibitor SAHA on viral reservoirs in SIV-infected Chinese rhesus macaques
22737073 2012 Animal Cohort PLoS Pathogens Highly intensified multidrug ART achieved long-term viral suppression and reservoir restriction in SIVmac251-infected macaques
21505294 2011 Animal Cohort AIDS (London) Gold compound auranofin, added to ART, restricted the viral reservoir and delayed rebound after ART suspension in SIV-infected macaques

Norway Market Information

Darunavir is currently not marketed in Norway; no authorization records are available in the evidence pack.

Safety Considerations

Please refer to the package insert for safety information.

Rank Disease Evidence Level Reason for Hold
2 Feline acquired immunodeficiency syndrome L4 The single supporting trial (NCT02770508) is a human Phase 4 boosted-darunavir HIV regimen study, not a feline/FIV study — likely a disease-ontology mapping error in the knowledge graph; requires engineering review before further consideration
3 Neurodevelopmental disorder with ataxic gait, absent speech, and decreased cortical white matter L5 No mechanistic rationale, no clinical or literature evidence — model score only
4 Obsolete familial combined hyperlipidemia L5 Mechanistically contradictory: darunavir (especially ritonavir-boosted regimens) is a known cause of dyslipidemia, making it a risk factor rather than a treatment; disease label is also flagged as obsolete

Conclusion and Next Steps

Decision: Hold

Rationale: The only candidate reaching decision stage S1 (SIV infection) is supported solely by preclinical macaque studies in which darunavir is one component of multi-drug regimens, not the subject of dedicated efficacy testing — this is L4 evidence with no clinical trials. The remaining three candidates carry either a likely data/ontology error, no mechanistic support, or a mechanistically contraindicated relationship, and are all rated Hold.

To proceed, the following is needed:

  • Darunavir-specific (monotherapy or defined-combination) efficacy data in SIV models, isolating its contribution from co-administered agents
  • Resolution of the suspected disease-ontology mapping error for "feline acquired immunodeficiency syndrome" (rank 2) before any further evaluation
  • TFDA/regulatory label data (warnings, contraindications, DDI) once available, to support S1 safety screening
  • Confirmed original indication and MOA data from DrugBank or product labeling, since both are currently data gaps

    Disclaimer

This content is for research purposes only and does not constitute medical advice. Clinical validation is required before any clinical application.



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