Compositions comprising lopinavir and treatment of conditions

A composition and disease technology, applied in the direction of drug combination, medical preparations containing active ingredients, skin diseases, etc., can solve problems such as no effect

Pending Publication Date: 2022-01-11
DOUGLAS PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Of particular note, Gantt et al found that loprevir and ritonavir, which one might expect to act in a similar manner to nelfinavir, had no effect

Method used

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  • Compositions comprising lopinavir and treatment of conditions
  • Compositions comprising lopinavir and treatment of conditions
  • Compositions comprising lopinavir and treatment of conditions

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0363] Example 1: Activity of lopinavir alone and 12:1 (w / w) lopinavir:ritonavir on HSV2 replication.

[0364] figure 1 A shows phase contrast images of the effect of HSV2 infection on the morphology of N-Tert keratinocytes exposed to DMSO control or 20 μM lopinavir for 48 hours. The cytopathic effect of the virus was clearly visible in HSV2-infected cells treated with DMSO when compared to uninfected controls. However, HSV2-infected cells treated with 20 μM lopinavir showed little cytopathic effect.

[0365] figure 1 B shows a graph of anti-HSV antibody immunostaining of these cells, demonstrating that the majority of HSV2-infected cells treated with DMSO stained strongly positive for the virus, whereas there was no signal in control virus-negative cells. Very few HSV2 positive cells were seen in infected cells exposed to 20 μM lopinavir for 48 hours.

[0366] figure 1 C shows quantification of the percentage of HSV2 positive cells detected by immunostaining. Analysis o...

example 2

[0367] Example 2: Activity of 12:1w / w Lop / Rit and nelfinavir on HSV2 replication.

[0368] While prior art (Gantt et al. (supra)) suggests that these compounds (lopinavir (alone or with ritonavir)) are ineffective, the HIV protease inhibitor nelfinavir may have When active, the inventors surprisingly found that lopinavir (alone or together with ritonavir) cleared the virus. Therefore, the inventors compared the activity of nelfinavir and the activity of the composition of 12:1 (w / w) lopinavir: ritonavir, and they were studying the use of these APIs in cancer therapy. This compound has been used for efficacy (unpublished work discussed above).

[0369] figure 2 A shows representative images of anti-HSV immunostained HSV2-infected N-Tert keratinocytes treated with the indicated concentrations of API as well as mixtures of different APIs. Three separate images from each treatment were analyzed.

[0370] figure 2 B shows that 2 μM and 5 μM nelfinavir are less effective on H...

example 3

[0371] Example 3: Toxicity of lopinavir alone, Lop / Rit and nelfinavir in virus negative N-Tert cells.

[0372] The inventors noticed that nelfinavir seemed to cause some toxicity to N-Tert host cells and decided to analyze the toxicity.

[0373] image 3 Via-1 cassette viability assays are shown for uninfected N-Tert keratinocytes treated for 48 hours with the indicated API concentrations and mixtures of the indicated APIs. As can be seen, up to 25 μM lopinavir alone or 20 μM 12:1 (w / w) lopinavir:ritonavir had little toxic effect on these cells, while 10 μM nelfinavir showed Significant toxicity was observed (reduced cell viability to <60%) and 20 μM nelfinavir showed stronger toxicity (reduced cell viability to about 40%).

[0374] in conclusion

[0375] These results indicated that 20 μM lopinavir or 12:1 w / w Lop / Rit was more effective on HSV2 replication than 2 μM or 5 μM nelfinavir and was comparable to 10 μM nelfinavir. However, 10 μM nelfinavir exhibited stronger non...

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PUM

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Abstract

Provided herein are methods and compositions for treating and / or inhibiting the development or progression of conditions caused by, or associated with, Herpes Simplex Virus (HSV) infection. In particular, provided are compositions comprising lopinavir alone, or lopinavir and ritonavir, methods for their manufacture; and the use of said pharmaceutical compositions as a medicament. In particular, pharmaceutical compositions are provided for use in treating and / or inhibiting the progression of HSV related conditions.

Description

technical field [0001] Provided herein are methods and compositions for treating conditions caused by or associated with herpes simplex virus (HSV) infection and / or inhibiting the development or progression of these conditions. In particular, there are provided compositions comprising lopinavir alone or lopinavir and ritonavir; methods for the manufacture of these compositions; and the use of said pharmaceutical compositions as medicaments. In particular, pharmaceutical compositions are provided for use in treating and / or inhibiting the progression of HSV-related disorders. Background technique [0002] Human herpesviruses (HHV) are large enveloped double-stranded DNA viruses, and all have the characteristic of establishing lifelong infection in humans. This is achieved by their ability to exist in the host as an asymptomatic latent infection (where the virus is dormant) or after activation as a lytic infection with associated symptoms. It is worth noting that more than 90...

Claims

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Application Information

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IPC IPC(8): A61K31/513A61K9/06A61K47/12A61K47/44A61P31/22A61P17/00A61K31/427
CPCA61K31/513A61K31/427A61P31/22A61P17/00A61K9/0014A61K9/0031A61K9/0034A61K47/12A61K47/44A61K9/06A61K2300/00A61P31/12A61K9/107A61K47/26A61K45/06A61K31/425A61K31/505
Inventor 伊恩·汉普森琳妮·汉普森费尔古斯·卡梅伦·比尼彼得·舒尔曼
Owner DOUGLAS PHARMA
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