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 31/045 - Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
A61K 31/08 - Ethers or acetals acyclic, e.g. paraformaldehyde
A61K 31/133 - Amines, e.g. amantadine having hydroxy groups, e.g. sphingosine
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A61K 31/164 - Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/366 - Lactones having six-membered rings, e.g. delta-lactones
A61K 31/4045 - Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/48 - Ergoline derivatives, e.g. lysergic acid, ergotamine
A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
A61K 31/593 - 9,10-Secocholestane derivatives, e.g. cholecalciferol, vitamin D3
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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.
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.
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 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/593 - 9,10-Secocholestane derivatives, e.g. cholecalciferol, vitamin D3
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 37/00 - Drugs for immunological or allergic disorders
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 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/4045 - Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
A61K 31/48 - Ergoline derivatives, e.g. lysergic acid, ergotamine
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/26 - Psychostimulants, e.g. nicotine, cocaine
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
A61K 31/48 - Ergoline derivatives, e.g. lysergic acid, ergotamine
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/593 - 9,10-Secocholestane derivatives, e.g. cholecalciferol, vitamin D3
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 37/00 - Drugs for immunological or allergic disorders
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 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/4045 - Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
A61K 31/48 - Ergoline derivatives, e.g. lysergic acid, ergotamine
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/26 - Psychostimulants, e.g. nicotine, cocaine
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
A61K 31/48 - Ergoline derivatives, e.g. lysergic acid, ergotamine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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.
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 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 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for 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 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
G01N 33/574 - Immunoassay; Biospecific binding assay; Materials therefor for 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 or acetals acyclic, e.g. paraformaldehyde
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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 or acetals acyclic, e.g. paraformaldehyde
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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.
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.
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.
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
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 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
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.
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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.
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