Methods and compositions for therapeutic treatment

A composition, a technique for therapeutic effect, applied in the field of neuraminidase inhibitors and sufficient to lower calcineurin

Inactive Publication Date: 2009-11-04
LIMERICK BIOPHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Other immunosuppressants (such as cyclosporine) also cause neurotoxicity leading to undesired side effects

Method used

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  • Methods and compositions for therapeutic treatment
  • Methods and compositions for therapeutic treatment
  • Methods and compositions for therapeutic treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0396] Example 1: Human Study of the Effects of Quercetin (Q) and Tacrolimus on Transplant Patients

[0397] An empirical trial of the effect of oral quercetin (Q) on the CNS effects of tacrolimus can be performed. Inclusion criteria included patients who had undergone liver, kidney, and heart transplantation and who exhibited neurotoxic events (such as seizures, tremors, headache, and visual abnormalities) under tacrolimus therapy. Preferably, these patients have no prior history of prior transplantation or CNS effects associated with tacrolimus. Exemplary dosing regimens for tacrolimus are provided in the table below.

[0398]

[0399] Due to interindividual variability in the pharmacokinetics of tacrolimus, it is necessary to individualize the dosing regimen to achieve optimal therapeutic effect. The dose of tacrolimus was adjusted daily to achieve trough concentrations of 15-20 and approximately 10 ng / mL in the first and subsequent two weeks, respectively. Blood samp...

Embodiment 2

[0401] Example 2: Human study of the effect of quercetin (Q) and tacrolimus on patients with atopic dermatitis

[0402] An empirical trial of the effect of oral quercetin (Q) on the CNS effects of tacrolimus can be performed. Inclusion criteria included patients with atopic dermatitis under treatment with PROTOPIC ointment (tacrolimus) and exhibiting neurotoxic events (such as seizures, tremors, visual abnormalities, etc. . . . ). Patients can apply PROTOPIC Ointment 0.03% or PROTOPIC Ointment 0.01% to the affected skin twice a day.

[0403] 100-500 mg of Q per capsule was formulated and provided to all subjects. In some trials, placebo capsules were also formulated. Subjects were instructed to complete a daily diary for 7 days and to continue their baseline treatment and daily activities. On approximately day 7, they are asked to start administration of 2 capsules of Q (200-1000 mg) twice daily (total Q daily dose 200-2000 mg) or an equal dose of placebo, preferably in a d...

Embodiment 3

[0404] Example 3: BTB transporter activators increase the efficacy of tacrolimus

[0405] animal: 8-9 week old Lewis and Brown Norway male rats were obtained from Charles River Laboratories. The general procedures for animal care and feeding refer to the National Research Council (NRC)'s Guide for the Care and Use of Laboratory Animals (Guide for the Care and Use of Laboratory Animals) (1996) and the Animal Welfare Standards (Animal Welfare Standards).

[0406] deal with: Lewis rats were treated with different single doses of LNS 0694 i.p. 30 minutes before a single i.v. injection of tacrolimus at a concentration of 1 mg / kg as described in the table below.

[0407]

Group

LNS 0694 TM (BTB to

transport protein activator) treatment

(IP)

FK506 processing

(IV)

1

baseline

(untreated control)

---------

2

50mg / kg

1mg / kg

3

150mg / kg

1mg / kg

4

300mg / kg ...

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PUM

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Abstract

Methods and compositions are described for the modulation of central nervous system and / or fetal effects of calcineurin inhibitors. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of calcineurin inhibitors out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide for the increase of efflux transporter activity at Blood-Tissue, blood-CSF and placental-maternal barriers to increase the efflux of calcineurin inhibitor from physiological compartments, including central nervous system and fetal compartments.

Description

[0001] cross reference [0002] This application claims U.S. Provisional Application No. 60 / 882306, filed December 28, 2006, U.S. Provisional Application No. 60 / 940375, filed May 25, 2007, and U.S. Provisional Application No. 60 / 953192, filed July 31, 2007 The priority of these documents is incorporated into this application by reference in its entirety. Background technique [0003] Although anatomical blood barrier structures, such as the blood-tissue barrier (BTB), function as, for example, a barrier that isolates the central nervous system from systemic blood circulation, medicinal substances often cross this barrier causing systemic side effects rather than produce the desired local effect. [0004] For example, Prograf - the leading immunosuppressant on the market to prevent transplant rejection - has been reported to cause neurotoxicity in approximately 55% of liver transplant recipients, including tremor, headache and other motor, Changes in mental status and sensor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/7048A61K31/436
CPCA61K31/436A61K45/06A61K31/7048A61K31/352A61P25/00A61P29/00A61P37/00A61P37/06A61P43/00A61K2300/00
Inventor W·罗宾斯
Owner LIMERICK BIOPHARMA INC
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