ritonavir

P1, N=17, Completed, Jiangsu HengRui Medicine Co., Ltd. | N=32 --> 17 | Trial completion date: Aug 2026 --> Oct 2025 | Trial primary completion date: Jun 2025 --> Oct 2025 | Recruiting --> Completed

Treatment of LS180 human colon adenocarcinoma cells, a commonly used human PXR (hPXR) experimental model, with a hPXR agonist (rifampicin, T0901317, SR12813, ritonavir, or paclitaxel) increased AOX1 mRNA expression by 5.2-, 10.2-, 4.7-, 2.2-, and 6.5-fold, respectively, and increased a prototypic hPXR target gene (CYP3A4 mRNA) expression by 9.5-, 13.5-, 7.2-, 3.4-, and 18.0-fold, respectively...It was abolished by actinomycin D, indicating the mRNA increase occurred by a transcriptional mechanism...Control analysis indicated that PCN increased mouse PXR-regulated Cyp3a11 mRNA and Cyp3a-mediated enzyme activity. Overall, our novel data provide evidence for a role of PXR in AOX1 gene expression.

In contrast, ritonavir, another HIV protease inhibitor, or raltegravir, an HIV integrase inhibitor, has no significant effect, indicating that inhibition of viral enzymes is not directly involved in the regulation of CLDN2 expression. Notably, SQV enhanced the cytotoxic effects of multiple anticancer agents, including doxorubicin, cisplatin, and SN-38, in lung adenocarcinoma cell line-derived spheroids and patient-derived organoids. We suggest that SQV improves chemoresistance by reducing CLDN2 expression and oxidative stress in lung adenocarcinoma.

P3, N=10, Completed, Soroka University Medical Center | N=30 --> 10 | Active, not recruiting --> Completed

Compared to those in the control group, the average daily egg production, eggshell thickness, oviduct weight, oviduct index, and the levels of luteinizing hormone, progesterone, and follicle-stimulating hormone were significantly higher in the Pal group...Furthermore, metabolomics analysis revealed that the levels of metabolites such as ritonavir, nicotinate riboside, and inosine were upregulated in the Pal group...These findings indicated that dietary Pal supplementation enhanced the production performance, antioxidant capacity, anti-inflammatory response, and reproductive function of laying hens. Therefore, these findings lay the foundation for the development of strategies and protocols for the inclusion of Pal in the diet of laying hens.

PBPK modeling predicted that ritonavir or erythromycin (strong and moderate CYP3A4 inhibitors) would increase ribociclib steady-state area under the concentration-time curve (AUC) by 1.84-fold or show no meaningful impact, respectively. Steady-state ribociclib AUC was estimated to decrease by 83% and 74% with rifampicin and efavirenz, strong and moderate CYP3A4 inducers, respectively. Ribociclib was estimated to increase CYP3A4 substrate midazolam exposure by 280%. Mild HI or mild/moderate RI did not show an apparent impact on ribociclib PK. Using relevant data and methodology for EBC patients, this analysis informed the approved ribociclib label of no dose adjustment for EBC patients with concomitant use of a moderate CYP3A inhibitor, any degree of HI, or mild/moderate RI, and a reduced 200 mg dose for patients with concomitant use of a strong CYP3A inhibitor or severe RI.

Besides, combination treatment with GLS4 and ritonavir elevates the frequencies of both peripheral blood IFNγ + NK cells and liver-resident IFNγ + CD8+ T cells in the pAAV/HBV1.2 hydrodynamic injection (HDI) model. Furthermore, GLS4 partially restores innate and adaptive immunity in vivo. This signifies a potentially effective strategy for achieving a functional cure for HBV infection.

Molecular docking study showed Elbasvir (1) to exhibit the strongest binding affinity (-8.1 kcal/mol), followed by Velpatasvir (2) (-7.6 kcal/mol), Daclatasvir (3) (-7.5 kcal/mol), Ritonavir (4) (-6.2 kcal/mol), Paliperidone Palmitate (5) (-5.9 kcal/mol), Saralasin (6) (-5.4 kcal/mol), Nystatin (8) (-5.2 kcal/mol), and Cobicistat (-5.1 kcal/mol)...Overall, the study provides mechanistic insights into the molecular interactions between FGF2 and these candidate drugs, highlighting the promising potential of compounds 1-6 and 8 for subsequent in vitro validation in cancer therapeutics. The online version contains supplementary material available at 10.1007/s40203-025-00495-2.

P1/2, N=862, Recruiting, DualityBio Inc. | Trial completion date: Jan 2028 --> May 2028 | Trial primary completion date: Sep 2027 --> Dec 2027

P1/2, N=750, Recruiting, DualityBio Inc. | Trial completion date: Sep 2026 --> Jan 2028 | Trial primary completion date: Sep 2026 --> Sep 2027

Finally, consistent with the key role that AKT and EMT play in OSCC radio-resistance, RTV increased OSCC cells' sensitivity to therapeutic doses of ionizing radiation. These preliminary in vitro findings encourage the use of RTV to prevent the malignant evolution of OPMDs, reduce the risk of OSCC metastasis, and improve the outcomes of anti-OSCC radiotherapy.

ALKBH2 overexpression is observed in many cancer and leads to temozolomide resistance in glioblastoma cell lines...Building on our previously reported finding that the HIV protease inhibitor ritonavir selectively binds and inhibits ALKBH2, we synthesized a BODIPY-labeled ritonavir (rit-BD) as an imaging agent...Furthermore, In vitro and in cellulo experiments and live-cell imaging confirmed that rit-BD could be used to label ALKBH2 in the living cell nucleus. Our findings establish rit-BD as a unique dual-purpose agent for visualizing ALKBH2 dynamics and inhibiting DNA repair activity in cancer cells.