Drug name
Last update: Sep 2025Lopinavir, Ritonavir, and Tenofovir (LRT) TLC-ART 101
Developer(s)
Drug information
- https://go.drugbank.com/drugs/DB14126
- https://go.drugbank.com/drugs/DB01601
- https://go.drugbank.com/drugs/DB00503
Lopinavir, Ritonavir, and Tenofovir
TLC-ART 101
Small molecule
protease inhibitors (PI) + nucleotide analog reverse-transcriptase inhibitor (NRTI)
The combination of lopinavir, ritonavir, and tenofovir is formulated using drug combination nanoparticle (DcNP) technology, allowing a single subcutaneous dose to last up to five weeks. Terminal half-lives are lopinavir (219 h), tenofovir (63 h), and lamivudine (136 h). TLC-ART101 inhibits HIV via multiple mechanisms: lopinavir and ritonavir as protease inhibitors, and tenofovir and lamivudine as reverse transcriptase inhibitors. DcNP loading is high for lopinavir and ritonavir (>90%) and moderate for tenofovir and lamivudine (~12–17%). Preclinical and clinical studies show substantial intracellular retention, i.e., lymph node mononuclear cells (LNMCs)-to-plasma ratios at 192 h: LPV: 102.8; RTV: 572.0; TFV: 2.9; and 3TC: 352.1
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Therapeutic area(s)
- HIV
- Treatment
Administration route
Subcutaneous
Associated long-acting platforms
Based on other organic particles, Aqueous drug particle suspension
Use of drug
- Administered by a community health worker
- Administered by a nurse
- Administered by a specialty health worker
- Monthly
- Every 2 weeks
Dosage
15.6 mg lopinavir; 4.1 mg ritonavir; 9.2 mg tenofovir
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Associated compounds, formulations and regimens
Not provided
Associated technologies
Not provided
Additional information
Developer(s)
University of Washington
The University of Washington was established in Seattle in 1861 to serve the Washington Territory. The UW developed into a major research institution, becoming the recipient of more federal research dollars than any other U.S. public university. UW has strong infrastructure for drug discovery, such as Center for clinical genomics, mass spectrometry center and preclinical research organization.
Drug structure
Scale-up and manufacturing prospects
Not provided
1. Spray dryer 2. High-shear mixers or homogenizers (for mixing and size reduction) 3. High-pressure homogenizer or microfluidizer 4. Sterile filtration units 5. Aseptic filling systems
1. Dissolve all drugs and lipids in ethanol (with minimal aqueous buffer) at 65–75 °C 2. Spray-dry the solution under controlled conditions (ProCepT or Buchi spray dryer) 3. Collect powder and convert to nanosuspension via homogenization 4. Add Excipients: DSPC and DSPE-PEG2000 5. Final product: Nanoparticles (~50–200 nm) with a multi-drug motif (MDM) structure
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Excipients & delivery device(s)
No proprietary excipient used
1. 1,2-Distearoyl-sn-glycero-3-phosphocholine (DSPC) 2. 1,2-Distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] (DSPE-PEG2000)
No residual solvent used
No delivery device
Safety, Efficacy and Evidence Summary
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Lopinavir, Ritonavir, and Tenofovir (LRT) combination, formulation, and method of administration
combination pharmaceutical compositions and methods thereof. The present invention relates to combination pharmaceutical compositions, which include a combination of hydrophilic and hydrophobic therapeutic agents (i.e., drugs) that are assembled together with excipients under specific conditions, forming a homogeneous pharmaceutical powder with multiple motif structure. unified repetitive drugs (mdm). Unlike currently available drug combination powders, which are amorphous, the combination pharmaceutical compositions (e.g., combination therapeutic agent powders) of the present invention have long-range order, in the form of unified, repetitive multidrug motifs. .
WO2020146788
Combination, Formulation
University Of Washington
Not provided
January 10, 2040
Pending: BR, CN, US