Methods and compositions for the treatment of cancer, tumors, and tumor-related disorders

a technology for cancer and tumors, applied in the field of combination compositions, can solve the problems of limited benefit of additional conventional treatment, serious and often life-threatening conditions of cancer, tumors, tumor-related disorders, etc., and achieve the effects of increasing or maintaining the same effect, decreasing the dosage, and increasing the therapeutic

Inactive Publication Date: 2013-04-04
ADASTRA PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This combination therapy increases the effectiveness of cancer treatment, reduces side effects, and prolongs the effectiveness of cancer therapies by minimizing drug resistance, while also simplifying treatment regimens and improving patient compliance.

Problems solved by technology

Cancer, tumors, tumor-related disorders, and neoplastic disease states are serious and often times life-threatening conditions.
If patients fail to respond to an erlotinib treatment, additional conventional treatment offers limited benefit.
Despite erlotinib's approval for the treatment of stage IIIB and IV non-small cell lung cancer, as with most therapeutic agents, side-effects result from its use.

Method used

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  • Methods and compositions for the treatment of cancer, tumors, and tumor-related disorders
  • Methods and compositions for the treatment of cancer, tumors, and tumor-related disorders
  • Methods and compositions for the treatment of cancer, tumors, and tumor-related disorders

Examples

Experimental program
Comparison scheme
Effect test

example 1

Synthesis of 2-(4-ethoxyphenyl)-4-methyl-1-(4-sulfamoylphenyl)-pyrrole

[0422]

[0423]Substituted benzaldehyde undergoes dehydration condensation by reaction with aniline compound A in an inert solvent at a temperature of between 5° C. to 200° C. to give aldimine compound B. Trimethylsilyl cyanide is then reacted with aldimine compound B in the presence of a Lewis acid to afford anilinonitrile C. An α-β-unsaturated aldehyde is then reacted with anilinonitrile C to afford compound D which then undergoes dehydration and dehydrogencyanation under basic conditions in a modification of the method described in Ann Chem. 589, 176 (1954).

example 2

Synthesis of Erlotinib

[0424]

[0425]Starting material compound H is heated in a suspension of metal alkali and solvent, then heated to give compound I. Starting material alcohol F, is placed in a solvent mixture of thionyl chloride, methylene chloride and dimethylformamide to give the chloride G. Chloride G is then coupled with compound I to give erlotinib J.

example 3

Pharmacokinetics and Metabolism of 2-(4-ethoxyphenyl)-4-methyl-1-(4-sulfamoylphenyl)-pyrrole

[0426]Orally administered 2-(4-ethoxyphenyl)-4-methyl-1-(4-sulfamoylphenyl)-pyrrole was rapidly absorbed in all species examined (mice, rats, dogs, and monkeys). Peak plasma concentrations were achieved between 1 and 3 hours after a dose of 5 mg / kg. The elimination half life (t1 / 2) was 4-5 hours in rodents and dogs, and approximately 2 hours in monkeys. Oral availability was greatest in rodent, and was reduced in dogs and monkeys (59 and 34% respectively). Pharmacokinetics in human subjects demonstrated a linear dose exposure relationship from doses of 2 mg to 800 mg given orally. The half-life in human subjects is 15-18 hours.

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Abstract

Described herein are compositions and methods for using these compositions in the treatment of cancer, tumors, and tumor-related disorders in a subject.

Description

CROSS-REFERENCE[0001]This application claims the benefit of U.S. Provisional Application No. 60 / 949,483, filed Jul. 12, 2007; U.S. Provisional Application No. 60 / 990,900, filed Nov. 28, 2007; and U.S. Provisional Application No. 61 / 044,425, filed Apr. 11, 2008, the contents of which are incorporated herein by reference in their entirety.FIELD[0002]The present invention relates to combination compositions and the use of such combinations for the treatment of cancer, tumors, and tumor-related disorders.BACKGROUND[0003]Cancer, tumors, tumor-related disorders, and neoplastic disease states are serious and often times life-threatening conditions. These diseases and disorders, which are characterized by rapidly-proliferating cell growth, continue to be the subject of research efforts directed toward the identification of therapeutic agents which are effective in the treatment thereof. Such agents prolong the survival of the patient, inhibit the rapidly-proliferating cell growth associated...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/402A61K31/517
CPCA61K31/05A61K31/352A61K31/402A61K31/4706A61K31/506A61K31/517A61K31/519A61K45/06A61K31/7068A61K31/5377A61K2300/00A61P35/00A61P35/02A61P43/00
InventorESTOK, THOMAS M.ZAKNOEN, SARA L.MANSFIELD, ROBERT K.LAWHON, TRACY
OwnerADASTRA PHARMA INC