A composition comprising an agonist of a 5-hydroxytryptamine (5-HT) receptor subtype 2A, 2B or 2C (5-HT2A, 5-HT2B or 5-HT2C), for the use in the treatment of a cognitive or neurological disorder in a patient, said patient having been pre-treated with naltrexone, or a metabolite thereof or an analogue selected from the group consisting of methylnaltrexone, nalmefene and nalorphine.
A composition comprising an agonist of a 5-hydroxytryptamine (5-HT) receptor subtype 3, for the use in the treatment of a cognitive or neurological disorder in a patient, said patient having been pre-treated with naltrexone, or a metabolite thereof or an analogue selected from the group consisting of methylnaltrexone, nalmefene and nalorphine.
A pharmaceutical composition comprising naltrexone or a metabolite thereof or an analogue selected from the group consisting of methylnaltrexone, nalmefene and nalorphine, for use in the treatment of an autoimmune disease within a subject, wherein a therapeutically effective amount of the naltrexone or metabolite thereof or analogue of either is to be administered to the subject in a first treatment phase, wherein after the first treatment phase the subject is to be administered a therapeutically effective amount of a cannabinoid, flavonoid or terpene in a second treatment phase, and wherein an agonist of a 5-hydroxytryptamine (5-HT) receptor is to be administered to the subject either simultaneously, sequentially or separately with the naltrexone, the metabolite or analogue.
A61K 31/164 - Amides, p.ex. acides hydroxamiques d'un acide carboxylique avec un aminoalcool, p.ex. céramides
A61K 31/165 - Amides, p.ex. acides hydroxamiques ayant des cycles aromatiques, p.ex. colchicine, aténolol, progabide
A61K 31/232 - Esters, p.ex. nitroglycérine, sélénocyanates d'acides carboxyliques d'acides acycliques, p.ex. pravastatine d'acides ayant un groupe carboxyle lié à une chaîne d'au moins sept atomes de carbone ayant au moins trois doubles liaisons, p.ex. étrétinate
A61K 31/343 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p.ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p.ex. isosorbide condensés avec un carbocycle, p.ex. coumarane, bufaralol, béfunolol, clobenfurol, amiodarone
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p.ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p.ex. cannabinols, méthanthéline
A61K 31/357 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p.ex. fungichromine ayant plusieurs atomes d'oxygène dans le même cycle, p.ex. éthers en couronne, guanadrel
A61K 31/366 - Lactones ayant des cycles à six chaînons, p.ex. delta-lactones
A61K 31/4045 - Indole-alkylamines; Leurs amides, p.ex. sérotonine, mélatonine
A61K 31/454 - Pipéridines non condensées, p.ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p.ex. pimozide, dompéridone
A61K 31/48 - Dérivés de l'ergoline, p.ex. acide lysergique, ergotamine
A61K 31/575 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrène; Leurs dérivés, p.ex. stéroïdes substitués en position 17 bêta par une chaîne d'au moins trois atomes de carbone, p.ex. cholane, cholestane, ergostérol, sitostérol
A61K 31/593 - Dérivés du 9,10-séco-cholestane, p.ex. cholécalciférol, vitamine D3
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p.ex. phosphate de pyridoxal
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p.ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
The invention is a single unit oral dose pharmaceutical composition comprising a first active ingredient and a second active ingredient;
wherein the first active ingredient is for absorption in the gastrointestinal tract from the oesophagus onwards;
wherein the second active ingredient is for absorption in the oral cavity; and
wherein the first active ingredient is naltrexone in an amount of 0.01 to 10 mg and the second active ingredient is calcitriol in an amount of 80 to 200 ug.
The invention is a single unit oral dose pharmaceutical composition comprising a first active ingredient and a second active ingredient;
wherein the first active ingredient is for absorption in the gastrointestinal tract from the oesophagus onwards;
wherein the second active ingredient is for absorption in the oral cavity; and
wherein the first active ingredient is naltrexone in an amount of 0.01 to 10 mg and the second active ingredient is calcitriol in an amount of 80 to 200 ug.
The pharmaceutical composition is particularly effective in the treatment of cancer.
The present invention provides novel therapeutic applications of low dose naltrexone (LDN). Said applications have been determined in light of the discovery by the present inventors that naltrexone acts as an antagonist of Toll-like receptor 9 (TLR9), an innate immune receptor which elicits the production of inflammatory cytokines when agonised. Chronic inflammation and TLR9 overexpression are characteristics of a number of disorders, including certain cancers. Accordingly, the present invention provides novel uses of naltrexone in the treatment of a subject having a disorder characterised by TLR9 overexpression and/or overactivity of TLR9-mediated signalling. The present invention also provides novel uses of naltrexone in the supportive care of subject having a tumour/cancer, and methods of treating and providing supportive care to a subject, comprising the administration of naltrexone.
A61K 39/39 - Préparations médicinales contenant des antigènes ou des anticorps caractérisées par les additifs immunostimulants, p.ex. par les adjuvants chimiques
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 31/593 - Dérivés du 9,10-séco-cholestane, p.ex. cholécalciférol, vitamine D3
The present invention relates to naltrexone or an analogue thereof, wherein the analogue is methylnaltrexone, naloxone, nalmefene and nalorphine and vitamin D or an active metabolite, or a pharmaceutically acceptable salt of either for separate, sequential or simultaneous administration, for use in the therapy of an autoimmune disease.
An in vitro method for identifying an anti-cancer agent, the therapeutic efficacy of which is enhanced upon administration with a second agent that increases the expression of OPRK1 and/or BAD, comprising the steps of:
(a) co-incubating a population of cells with a target anti-cancer agent and said second agent and
(b) measuring the cytotoxicity and/or cytostasis in the population of cells;
wherein the therapeutic efficacy of the target anti-cancer agent is enhanced if the cytotoxicity and/or cytostasis of the target anti-cancer agent is increased compared to a control.
G01N 33/50 - Analyse chimique de matériau biologique, p.ex. de sang ou d'urine; Test par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligands; Test immunologique
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A single unit oral dose pharmaceutical composition for use as a medicament for separate, sequential or simultaneous administration with an agonist of a 5- hydroxytryptamine (5-HT) receptor; wherein the single unit oral dose pharmaceutical composition comprises a first active ingredient and a second active ingredient; wherein the first active ingredient is for absorption in the gastrointestinal tract from the oesophagus onwards and the second active ingredient is for absorption in the oral cavity; and wherein the first active ingredient is naltrexone in an amount of 0.01 to 10 mg and the second active ingredient is calcitriol in an amount of 80 to 200 ug.
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 31/593 - Dérivés du 9,10-séco-cholestane, p.ex. cholécalciférol, vitamine D3
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
A61P 1/00 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p.ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
A61P 37/00 - Médicaments pour le traitement des troubles immunologiques ou allergiques
9.
COMPOSITIONS COMPRISING AN AGONIST OF 5-HYDROXYTRYPTAMINE (5-HT) RECEPTOR SUBTYPE 3
A composition comprising an agonist of a 5-hydroxytryptamine (5-HT) receptor subtype 3, for the use in the treatment of a cognitive or neurological disorder in a patient, said patient having been pre-treated with naltrexone, or a metabolite thereof or an analogue selected from the group consisting of methylnaltrexone, nalmefene and nalorphine.
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 31/4045 - Indole-alkylamines; Leurs amides, p.ex. sérotonine, mélatonine
A61K 31/48 - Dérivés de l'ergoline, p.ex. acide lysergique, ergotamine
A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p.ex. azélastine, pentylènetétrazole
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p.ex. phosphate de pyridoxal
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p.ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
10.
NALTREXONE FOR IMPROVING THE EFFECTIVENESS OF 5-HT RECEPTOR SUBTYPE 2A, 2B OR 2C AGONISTS
A composition comprising an agonist of a 5-hydroxytryptamine (5-HT) receptor subtype 2A, 2B or 2C (5-HT2A, 5-HT2B or 5-HT2C), for the use in the treatment of a cognitive or neurological disorder in a patient, said patient having been pre- treated with naltrexone, or a metabolite thereof or an analogue selected from the group consisting of methylnaltrexone, nalmefene and nalorphine.
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 31/135 - Amines, p.ex. amantadine ayant des cycles aromatiques, p.ex. méthadone
A61K 31/36 - Composés contenant des groupes méthylènedioxyphényle, p.ex. sésamine
A61K 31/48 - Dérivés de l'ergoline, p.ex. acide lysergique, ergotamine
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p.ex. phosphate de pyridoxal
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p.ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
11.
NALTREXONE FOR BOOSTING THE THERAPEUTIC UTILITY OF 5-HT RECEPTOR AGONISTS
A single unit oral dose pharmaceutical composition for use as a medicament for separate, sequential or simultaneous administration with an agonist of a 5- hydroxytryptamine (5-HT) receptor; wherein the single unit oral dose pharmaceutical composition comprises a first active ingredient and a second active ingredient; wherein the first active ingredient is for absorption in the gastrointestinal tract from the oesophagus onwards and the second active ingredient is for absorption in the oral cavity; and wherein the first active ingredient is naltrexone in an amount of 0.01 to 10 mg and the second active ingredient is calcitriol in an amount of 80 to 200 ug.
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 31/593 - Dérivés du 9,10-séco-cholestane, p.ex. cholécalciférol, vitamine D3
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
A61P 1/00 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p.ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
A61P 37/00 - Médicaments pour le traitement des troubles immunologiques ou allergiques
A pharmaceutical composition comprising naltrexone or a metabolite thereof or an analogue selected from the group consisting of methylnaltrexone, nalmefene and nalorphine, for use in the treatment of an autoimmune disease within a subject, wherein a therapeutically effective amount of the naltrexone or metabolite thereof or analogue of either is to be administered to the subject in a first treatment phase, wherein after the first treatment phase the subject is to be administered a therapeutically effective amount of a cannabinoid, flavonoid or terpene in a second treatment phase, and wherein an agonist of a 5- hydroxytryptamine (5-HT) receptor is to be administered to the subject either simultaneously, sequentially or separately with the naltrexone, the metabolite or analogue.
A pharmaceutical composition comprising naltrexone or a metabolite thereof or an analogue selected from the group consisting of methylnaltrexone, nalmefene and nalorphine, for use in the treatment of an autoimmune disease within a subject, wherein a therapeutically effective amount of the naltrexone or metabolite thereof or analogue of either is to be administered to the subject in a first treatment phase, wherein after the first treatment phase the subject is to be administered a therapeutically effective amount of a cannabinoid, flavonoid or terpene in a second treatment phase, and wherein an agonist of a 5- hydroxytryptamine (5-HT) receptor is to be administered to the subject either simultaneously, sequentially or separately with the naltrexone, the metabolite or analogue.
A composition comprising an agonist of a 5-hydroxytryptamine (5-HT) receptor subtype 3, for the use in the treatment of a cognitive or neurological disorder in a patient, said patient having been pre-treated with naltrexone, or a metabolite thereof or an analogue selected from the group consisting of methylnaltrexone, nalmefene and nalorphine.
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 31/4045 - Indole-alkylamines; Leurs amides, p.ex. sérotonine, mélatonine
A61K 31/48 - Dérivés de l'ergoline, p.ex. acide lysergique, ergotamine
A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p.ex. azélastine, pentylènetétrazole
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p.ex. phosphate de pyridoxal
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p.ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
15.
NALTREXONE FOR IMPROVING THE EFFECTIVENESS OF 5-HT RECEPTOR SUBTYPE 2A, 2B OR 2C AGONISTS
A composition comprising an agonist of a 5-hydroxytryptamine (5-HT) receptor subtype 2A, 2B or 2C (5-HT2A, 5-HT2B or 5-HT2C), for the use in the treatment of a cognitive or neurological disorder in a patient, said patient having been pre- treated with naltrexone, or a metabolite thereof or an analogue selected from the group consisting of methylnaltrexone, nalmefene and nalorphine.
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p.ex. phosphate de pyridoxal
A61K 31/135 - Amines, p.ex. amantadine ayant des cycles aromatiques, p.ex. méthadone
A61K 31/36 - Composés contenant des groupes méthylènedioxyphényle, p.ex. sésamine
A61K 31/48 - Dérivés de l'ergoline, p.ex. acide lysergique, ergotamine
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p.ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
The present invention is based on the finding that the inhibition of the proliferation of cancer cells by cannabinoids is brought about more effectively by combined treatment with low dose naltrexone (LDN) or 6-β-naltrexone (6BN), a metabolite of naltrexone. There is provided a pharmaceutical composition comprising naltrexone or a metabolite thereof or an analogue thereof, for use in the treatment of an autoimmune disease within a subject, wherein a therapeutically effective amount of the naltrexone or metabolite thereof or analogue of either is to be administered to the subject in a first treatment phase, wherein after the first treatment phase the subject is to be administered a therapeutically effective amount of a cannabinoid in a second treatment phase.
The invention is a single unit oral dose pharmaceutical composition comprising a first active ingredient and a second active ingredient; wherein the first active ingredient is for absorption in the gastrointestinal tract from the oesophagus onwards; wherein the second active ingredient is for absorption in the oral cavity; and wherein the first active ingredient is naltrexone in an amount of 0.01 to 10 mg and the second active ingredient is calcitriol in an amount of 80 to 200 ug. The pharmaceutical composition is particularly effective in the treatment of cancer.
A61K 9/19 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres lyophilisées
A61K 9/24 - Pilules, pastilles ou comprimés du type à libération prolongée ou discontinue en doses unitaires constituées de couches ou feuilletées
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 31/593 - Dérivés du 9,10-séco-cholestane, p.ex. cholécalciférol, vitamine D3
A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/42 - Protéines; Polypeptides; Leurs produits de dégradation; Leurs dérivés p.ex. albumine, gélatine ou zéine
The invention is a single unit oral dose pharmaceutical composition comprising a first active ingredient and a second active ingredient; wherein the first active ingredient is for absorption in the gastrointestinal tract from the oesophagus onwards; wherein the second active ingredient is for absorption in the oral cavity; and wherein the first active ingredient is naltrexone in an amount of 0.01 to 10 mg and the second active ingredient is calcitriol in an amount of 80 to 200 ug. The pharmaceutical composition is particularly effective in the treatment of cancer.
A61K 9/24 - Pilules, pastilles ou comprimés du type à libération prolongée ou discontinue en doses unitaires constituées de couches ou feuilletées
A61K 9/19 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres lyophilisées
A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/42 - Protéines; Polypeptides; Leurs produits de dégradation; Leurs dérivés p.ex. albumine, gélatine ou zéine
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 31/593 - Dérivés du 9,10-séco-cholestane, p.ex. cholécalciférol, vitamine D3
The invention relates to a method for monitoring the treatment of a subject undergoing therapy with an active that is naltrexone or a metabolite or analogue thereof, comprising:
a. measuring the level of pERK in a sample obtained from the subject undergoing treatment;
b. comparing the level of pERK with a reference,
wherein if the pERK level is increased compared to the reference, then the active is being administered at an effective level.
The invention relates to a method for monitoring the treatment of a subject undergoing therapy with an active that is naltrexone or a metabolite or analogue thereof, comprising:
measuring the gene expression profile of any of the genes listed in Table 1 or Table 2, in a sample of CD3+ cells obtained from the subject undergoing treatment;
wherein if the expression of any of the genes in Table 1 is increased compared to a control, or if any of the genes listed in Table 2 is decreased compared to a control the active is being administered at an effective level.
C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p.ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
21.
CANCER TREATMENT COMPRISING NALTREXONE AND A CANNABINOID
The present invention is based on the finding that the inhibition of the proliferation of cancer cells by cannabinoids is brought about more effectively by combined treatment with low dose naltrexone (LDN) or 6-β-naltrexone (6BN), a metabolite of naltrexone. There is provided a pharmaceutical composition comprising naltrexone or a metabolite thereof or an analogue thereof, for use in the treatment of cancer within a subject, wherein a therapeutically effective amount of the naltrexone or metabolite thereof or analogue of either is to be administered to the subject in a first treatment phase, wherein after the first treatment phase the subject is to be administered a therapeutically effective amount of a cannabinoid in a second treatment phase, and wherein the subject is to be administered a chemotherapeutic agent before, during or following the treatment.
The disclosure provides methods of treating a tumor/cancer by administering naltrexone or an analogue thereof, followed by a recovery phase, and then administering a small molecule signaling inhibitor such as PI3-kinase inhibitors, AKT inhibitors, taxanes, antimetabolites, alkylating agents and/or cell cycle inhibitors. The disclosure also provides diagnostic methods for assessing a therapeutic response to the methods of treatment.
A61K 31/436 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à six chaînons ayant l'oxygène comme hétéro-atome du cycle, p.ex. rapamycine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p.ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p.ex. cytidine, acide cytidylique
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
G01N 33/574 - Tests immunologiques; Tests faisant intervenir la formation de liaisons biospécifiques; Matériaux à cet effet pour le cancer
The present invention relates to naltrexone or an analogue thereof, wherein the analogue is methylnaltrexone, naloxone, nalmefene and nalorphine and vitamin D or an active metabolite, or a pharmaceutically acceptable salt of either for separate, sequential or simultaneous administration, for use in the therapy of an autoimmune disease.
The present invention is based on the finding that the inhibition of the proliferation of cancer cells by cannabinoids is brought about more effectively by combined treatment with low dose naltrexone (LDN) or 6-β-naltrexone (6BN), a metabolite of naltrexone. There is provided a pharmaceutical composition comprising naltrexone or a metabolite thereof or an analogue thereof, for use in the treatment of cancer within a subject, wherein a therapeutically effective amount of the naltrexone or metabolite thereof or analogue of either is to be administered to the subject in a first treatment phase, wherein after the first treatment phase the subject is to be administered a therapeutically effective amount of a cannabinoid in a second treatment phase.
The present invention is based on the finding that the inhibition of the proliferation of cancer cells by cannabinoids is brought about more effectively by combined treatment with low dose naltrexone (LDN) or 6-β-naltrexone (6BN), a metabolite of naltrexone. There is provided a pharmaceutical composition comprising naltrexone or a metabolite thereof or an analogue thereof, for use in the treatment of cancer within a subject, wherein a therapeutically effective amount of the naltrexone or metabolite thereof or analogue of either is to be administered to the subject in a first treatment phase, wherein after the first treatment phase the subject is to be administered a therapeutically effective amount of a cannabinoid in a second treatment phase, and wherein the subject is to be administered a chemotherapeutic agent before, during or following the treatment.
A61K 31/08 - Ethers ou acétals acycliques, p.ex. paraformaldéhyde
A61K 31/192 - Acides carboxyliques, p.ex. acide valproïque ayant des groupes aromatiques, p.ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p.ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p.ex. cannabinols, méthanthéline
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p.ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p.ex. cytidine, acide cytidylique
26.
CANCER TREATMENT COMPRISING NALTREXONE AND A CANNABINOID
The present invention is based on the finding that the inhibition of the proliferation of cancer cells by cannabinoids is brought about more effectively by combined treatment with low dose naltrexone (LDN) or 6-ß-naltrexone (6BN), a metabolite of naltrexone. There is provided a pharmaceutical composition comprising naltrexone or a metabolite thereof or an analogue thereof, for use in the treatment of cancer within a subject, wherein a therapeutically effective amount of the naltrexone or metabolite thereof or analogue of either is to be administered to the subject in a first treatment phase, wherein after the first treatment phase the subject is to be administered a therapeutically effective amount of a cannabinoid in a second treatment phase, and wherein the subject is to be administered a chemotherapeutic agent before, during or following the treatment.
A61K 31/08 - Ethers ou acétals acycliques, p.ex. paraformaldéhyde
A61K 31/192 - Acides carboxyliques, p.ex. acide valproïque ayant des groupes aromatiques, p.ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p.ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p.ex. cannabinols, méthanthéline
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p.ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p.ex. cytidine, acide cytidylique
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p.ex. composés antiphlogistiques et pour le cœur
The invention relates to a method for monitoring the treatment of a subject undergoing therapy with an active that is naltrexone or a metabolite or analogue thereof, comprising: measuring the gene expression profile of any of the genes listed in Table or Table 2, in a sample of CD3+ cells obtained from the subject undergoing treatment; wherein if the expression of any of the genes in Table 1 is increased compared to a control, or if any of the genes listed in Table 2 is decreased compared to a control the active is being administered at an effective level.
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
G01N 33/53 - Tests immunologiques; Tests faisant intervenir la formation de liaisons biospécifiques; Matériaux à cet effet
C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismes; Compositions à cet effet; Procédés pour préparer ces compositions faisant intervenir des acides nucléiques
The invention relates to a method for monitoring the treatment of a subject undergoing therapy with an active that is naltrexone or a metabolite or analogue thereof, comprising: a.measuring the level of pERK in a sample obtained from the subject undergoing treatment; b.comparing the level of pERK with a reference, wherein if the pERK level is increased compared to the reference,then the active is being administered at an effective level.
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
G01N 33/68 - Analyse chimique de matériau biologique, p.ex. de sang ou d'urine; Test par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligands; Test immunologique faisant intervenir des protéines, peptides ou amino-acides
G01N 33/50 - Analyse chimique de matériau biologique, p.ex. de sang ou d'urine; Test par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligands; Test immunologique
wherein the therapeutic efficacy of the target anti-cancer agent is enhanced if the cytotoxicity and/or cytostasis of the target anti-cancer agent is increased compared to a control.
G01N 33/50 - Analyse chimique de matériau biologique, p.ex. de sang ou d'urine; Test par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligands; Test immunologique
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
The present invention provides an agent that increases the expression of BAD, for use in the treatment of cancer in conjunction with a chemotherapeutic agent wherein the agent is selected from the list consisting of 6-β-naltrexol, naloxone, methyl naltrexone, or pharmaceutically acceptable salts thereof.
The invention is based on the finding that co-administration of 6-β-naltrexol alongside vitamin D together with a chemotherapeutic agent, results in a further reduction in lung cancer cell growth. The combination of 6-β-naltrexol with vitamin D results in a greater decrease in the growth of cancer cells compared to the sum of the effects of each agent when administered in isolation.
It has been found by the present inventors that agents that boost the expression of the opioid receptor kappa 1 (OPRK1) can enhance the cytotoxicity of chemotherapeutic agents in multiple cancer cell lines. Furthermore, the effect is dose dependent, where the greater the induced expression of OPRK1, the greater the cytotoxicity of the chemotherapeutic agent. The increase in overall cytotoxicity is independent of the cytotoxicity of the agent that increases the expression of OPRK1, which itself has no or minimal cytotoxic effect.
The present invention provides an agent that increases the expression of BAD, for use in the treatment of cancer in conjunction with a chemotherapeutic agent wherein the agent is selected from the list consisting of 6-.beta.-naltrexol, naloxone, methylnaltrexone, or pharmaceutically acceptable salts thereof.
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p.ex. phosphate de pyridoxal
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p.ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p.ex. cytidine, acide cytidylique
G01N 33/50 - Analyse chimique de matériau biologique, p.ex. de sang ou d'urine; Test par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligands; Test immunologique
The present invention relates to naltrexone or an analogue thereof, wherein the analogue is methylnaltrexone, naloxone, nalmefene and nalorphine and vitamin D or an active metabolite, or a pharmaceutically acceptable salt of either for separate, sequential or simultaneous administration, for use in the therapy of an autoimmune disease.
The present invention is based on the finding that the inhibition of the proliferation of cancer cells by cannabinoids is brought about more effectively by combined treatment with low dose naltrexone (LDN) or 6-ß-naltrexone (6BN), a metabolite of naltrexone. There is provided a pharmaceutical composition comprising naltrexone or a metabolite thereof or an analogue thereof, for use in the treatment of cancer within a subject, wherein a therapeutically effective amount of the naltrexone or metabolite thereof or analogue of either is to be administered to the subject in a first treatment phase, wherein after the first treatment phase the subject is to be administered a therapeutically effective amount of a cannabinoid in a second treatment phase.
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p.ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p.ex. cannabinols, méthanthéline
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
The present invention is based on the finding that the inhibition of the proliferation of cancer cells by cannabinoids is brought about more effectively by combined treatment with low dose naltrexone (LDN) or 6-β-naltrexone (6BN), a metabolite of naltrexone. There is provided a pharmaceutical composition comprising naltrexone or a metabolite thereof or an analogue thereof, for use in the treatment of cancer within a subject, wherein a therapeutically effective amount of the naltrexone or metabolite thereof or analogue of either is to be administered to the subject in a first treatment phase, wherein after the first treatment phase the subject is to be administered a therapeutically effective amount of a cannabinoid in a second treatment phase.
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p.ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p.ex. cannabinols, méthanthéline
A61K 31/485 - Dérivés du morphinane, p.ex. morphine, codéine
The invention is based on the finding that co-administration of 6-β-naltrexol alongside vitamin D together with a chemotherapeutic agent, results in a further reduction in lung cancer cell growth. The combination of 6-β-naltrexol with vitamin D results in a greater decrease in the growth of cancer cells compared to the sum of the effects of each agent when administered in isolation.
An in vitro method for identifying an anti-cancer agent, the therapeutic efficacy of which is enhanced upon administration with a second agent that increases the expression of OPRK1 and/or BAD, comprising the steps of: a. co-incubating a population of cells with a target anti-cancer agent and said second agent and b. measuring the cytotoxicity and/or cytostasis in the population of cells; wherein the therapeutic efficacy of the target anti-cancer agent is enhanced if the cytotoxicity and/or cytostasis of the target anti-cancer agent is increased compared to a control.
G01N 33/50 - Analyse chimique de matériau biologique, p.ex. de sang ou d'urine; Test par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligands; Test immunologique
39.
AN AGENT THAT INCREASES THE EXPRESSION OF THE OPIOID KAPPA 1 FOR THE TREATMENT OF CANCER
It has been found by the present inventors that agents that boost the expression of the opioid receptor kappa 1 (OPRK1) can enhance the cytotoxicity of chemotherapeutic agents in multiple cancer cell lines. Furthermore, the effect is dose dependent, where the greater the induced expression of OPRK1, the greater the cytotoxicity of the chemotherapeutic agent. The increase in overall cytotoxicity is independent of the cytotoxicity of the agent that increases the expression of OPRK1, which itself has no or minimal cytotoxic effect.
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p.ex. phosphate de pyridoxal
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p.ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p.ex. cytidine, acide cytidylique
G01N 33/50 - Analyse chimique de matériau biologique, p.ex. de sang ou d'urine; Test par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligands; Test immunologique
The present invention provides an agent that increases the expression of BAD, for use in the treatment of cancer in conjunction with a chemotherapeutic agent wherein the agent is selected from the list consisting of 6-β-naltrexol, naloxone, methylnaltrexone, or pharmaceutically acceptable salts thereof.
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p.ex. phosphate de pyridoxal
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p.ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p.ex. cytidine, acide cytidylique
G01N 33/50 - Analyse chimique de matériau biologique, p.ex. de sang ou d'urine; Test par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligands; Test immunologique
The present invention provides novel therapeutic applications of low dose naltrexone (LDN). Said applications have been determined in light of the discovery by the present inventors that naltrexone acts as an antagonist of Toll-like receptor 9 (TLR9), an innate immune receptor which elicits the production of inflammatory cytokines when agonised. Chronic inflammation and TLR9 overexpression are characteristics of a number of disorders, including certain cancers. Accordingly, the present invention provides novel uses of naltrexone in the treatment of a subject having a disorder characterised by TLR9 overexpression and/or overactivity of TLR9-mediated signalling. The present invention also provides novel uses of naltrexone in the supportive care of subject having a tumour/cancer, and methods of treating and providing supportive care to a subject, comprising the administration of naltrexone.
brevets
