Latest research on Lopinavir

Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. It is marketed by Abbott as Kaletra, a co-formulation with a sub-therapeutic dose of ritonavir, as a component of combination therapy to treat HIV/AIDS.

Latest findings

Specifically, Ethanol binding to CYP3A4 active site via non-covalent interaction with the heme iron decreases the maximum spectral binding change for Lopinavir and saquinavir [12]. [source, 2016]
We originally speculated that HIV protease inhibitors (PIs) may have activity against HPV related cervical disease and identified Lopinavir as the most effective [13] although this was at ten times the concentration achieved by oral dosing for HIV therapy [14]. [source, 2016]
Indeed, recent work has shown that oral Lopinavir, as used for normal HIV therapy, has little effect on HPV status in HIV positive women [15]. [source, 2016]
Subsequent in vitro studies defined at least part of the mode-of-action of Lopinavir against HPV [16] and many HIV PI’s are now well known to have more general anticancer properties [17,18,19]. [source, 2016]
Most notably, it has been suggested that Ritonavir (usually co-administred with lopinavir as Lopimune or Kaletra) may have anti-invasive and anti-proliferative activity against cells derived from pre-invasive CINs but little activity against cells derived from more advanced ICC [20]. [source, 2016]
Based on our pre-clinical studies it was concluded that direct application of Lopinavir to the cervix as a vaginal pessary or gel, might achieve the concentration required for activity against HPV related cervical dysplasia. [source, 2016]
Since we already had research collaborations in place with clinicians at Kenyatta National Hospital/University of Nairobi in Kenya, we built on these to conduct a trial of self-applied Lopinavir (in the form of Lopimune) in this setting with the aim of developing an effective, inexpensive, non-surgical, self-applied treatment with minimal side effects. [source, 2016]
Lopinavir was extracted from plasma using a method based on that of Djerada et al [25]. [source, 2016]
Standard amounts of ultrapure research grade Lopinavir (Santa Cruz Biotechnology, Inc. Heidelberg, GMBH) comprising 1000, 500, 100, 50, 25, 12.5 and 6.25ng were added to control plasma and extracted as above. [source, 2016]
All test plasma extractions and assays were performed in triplicate and were assayed with Lopinavir control standards. [source, 2016]