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GB2140686A - Drugs containing a psoralene derivative - Google Patents
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GB2140686A - Drugs containing a psoralene derivative - Google Patents

Drugs containing a psoralene derivative Download PDF

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Publication number
GB2140686A
GB2140686A GB08315070A GB8315070A GB2140686A GB 2140686 A GB2140686 A GB 2140686A GB 08315070 A GB08315070 A GB 08315070A GB 8315070 A GB8315070 A GB 8315070A GB 2140686 A GB2140686 A GB 2140686A
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GB
United Kingdom
Prior art keywords
drugs
treatment
active substance
methoxypsoralene
cancerous
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
GB08315070A
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GB8315070D0 (en
GB2140686B (en
Inventor
Jean-Jacques Goupil
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Individual
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Individual
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Publication date
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Publication of GB8315070D0 publication Critical patent/GB8315070D0/en
Publication of GB2140686A publication Critical patent/GB2140686A/en
Application granted granted Critical
Publication of GB2140686B publication Critical patent/GB2140686B/en
Expired legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/366Lactones having six-membered rings, e.g. delta-lactones
    • A61K31/37Coumarins, e.g. psoralen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Compositions for topical and oral application contain as an active substance 5-methoxypsoralene of the formula: <IMAGE> are useful for the treatment of epidermal proliferation tumours.

Description

SPECIFICATION Drugs containing a psoralene derivative This invention relates to new compositions of drugs containing as an active substance 5methoxypsoralene of the formula:
French Patent No. 77.31719 filed on October 21, 1977 in the name of the present applicant disclosed these new drugs as having a very high therapeutic index due to the very low toxicity of 5methoxypsoralene compared to that of other psoralenes. The Patent made clear that one could use therapeutic doses of 5-methoxypsoralene up to five times greater than those used for the 8methoxypsoralene and advocated the administration of oral doses of 20 mg to 300 mg of 5-methoxypsoralene per day, followed by a daily exposure to ultraviolet A, at a rate of 1.5 to 10 joules/cm2.
For topical administration, the patent advocated 5-methoxypsora lene concentrations between 100 ppm and 1000 ppm. Trials concerning the therapeutic activity of the new drugs had been carried out in the treatment of psoriasis, vitiligo, atypical eczema and mycosis fungoides.
It should be recalled here that mycosis fungoides is a well known skin cancer of the lymphoma type which is characterised by the proliferation of lymphocyte cells which are abundant in the lymph, that is, the interstitiai liquid irrigating notably the dermis and epidermis.
The clinical trials and experiments which were the basis of Patent No. 77 31719 were, of course, conducted both on patients affected with psoriasis and patients affected with skin cancer, since both of these illnesses are characterized by a more rapid than normal proliferation phenomenon of the cutaneous cells. This rapid proliferation phenomenon of the cells occurs at the level of the deoxyribonucleic acid (DNA) molecules present in the cell nucleus.
It is known that 5-methoxypsoralene, under the energetic action of UV.A radiation, attaches to each of the two helixes of a DNA molecule and so blocks the transcription process. No messenger RNA (ribonucleic acid) is manufactured, completely inhibiting protein synthesis and cell multiplication. In normal cells, the blocking of the DNA helixes is overcome by the faster action of the DNA self-repair systems. This is achieved either by excision or by replication.
But in the case of cells affected with psoriasis or cancer, that is cells where the multiplication phenomena are very accelerated, the self-repair systems do not have time to set to work. In the same cells however the psoralene, by forming bridges between the two DNA helixes, stops the anarchical cellular multiplication. This explains why 5-methoxypsoralene does not in any way disturb the multiplication of normal cells but selectively blocks diseased cells which are undergoing accelerated proliferation such as psoriatic cells or cancerous cells.
After the satisfactory results obtained with the treatment of the mycosis fungoides iymphoma (cancer of the lymph cells) by administration of 5methoxypsoralene and UV.A exposure, the applicant had the idea of carrying on with investigations on other types of cancers or precancerous lesions of the skin, that is, proliferation tumours of epidermal cells and not the proliferation of cells of the interstitial fluid such as the baso-cellular epithelioma, the spino-cellular epithelioma, Hutchinson's freckles, actinic hyperkeratosis and cutaneous melanomas, etc.
Such an idea was contrary to the well established view that therapy combining the use of 5-methoxypsoralene and UV.A irradiation was totally inadvisable in the case of epidermal proliferation tumours, since it was the solar radiation itself which produced such tumours.
It is therefore quite unexpected that the applicant found that 5-methoxypsoralene could heal malignant epidermal proliferation tumours when administered under new and special conditions; notably as regards posology.
The pharmacological activity of the drug was brought to the fore by topical administration of 5methoxypsoralene on mice having cancerous tumours produced by ultraviolet radiation.
It appeared that the concentrations of 5methoxypsoralene necessary for topical preparation were very high; from 10 to 100 times more than the prior art concentrations, and this as a function of the excipient.
The general toxicity of topical preparations having 1,000 to 10,000 ppm of 5methoxypsoralene has been studied in mice with various excipients, and has shown that the active substance is well tolerated, even in such high doses. This corresponds to the fact that 5methoxypsoralene is far less toxic than 8methoxypsoralene.
For the topical administration of 5methoxypsoralene, various carriers have proven satisfactory. The following examples are given by way of illustrations and are not limiting: -pure petroleum jellies of various viscosities of Codex, -modified petroleum jellies as the salycilated petroleum jelly, -mineral oils, -vegetable oils, particularly ethylenic oils comprising a small number of double bonds, -lanoline, -oily continuous phase emulsions, -alcoholic solutions, etc.
Due to the powerful barrier developed by the cancerous cells with regards to their environment, and notably the thickening phenomenon of the cellular membranes, the penetration of the drug by the topical route is slow and difficult.
According to the invention, it has been found that is was advantageous to introduce topical preparation penetration agents into the 5methoxypsoralene such as: -isopropyl myristate, -dimethyl sulphoxide (DMSO), etc.
The following clinical trials have been carried out with preparations containing 10,000 ppm of 5-methoxypsoralene in pure petroleum jelly.
All voluntary patients (a hundred of them) had family histories and personal histories of a skin cancer. They had all previously had many ablations of skin cancers, and all the previous treatments had not checked the formation of recurrent cancers.
The types of cancers of pre-cancerous lesions of these patients, which had been histologically proven were the following: -baso-cellular epitheliomas, -spino-cellular epitheliomas, -Hutchinson freckles actinic hyperkeratoses.
Some of these patients showed bilateral effects on the body or limbs so allowing a control to be set up, that is one side of the body or one limb received treatment and the other remained untreated.
All the patients chosen had no other serious illness.
All patients were treated for five weeks in the following manner: Twice a week, a pure petroleum jelly based preparation containing 10,000 ppm of 5methoxypsoralene was applied to the tumour and to its periphery (1 to 2 cm beyond the clinically evaluated limit of the tumour). From one to three hours after this application, the patient was subjected to an UV.A exposure with an energy of 5 joules/cm2 to 1 0 joules/cm2 (at the end of the treatment) after having re-applied the product a quarter of an hour prior to the exposure. The irradiation was applied to the whole area to which the 5-methoxypsoralene preparation had been applied.
The results were as follows: The biopsies carried out at the end of the treatment, that is from the sixth week and later, showed a total necrosis of the tumour's cancerous cells (as well as healing of the normal tissues).
Biopsies were carried out every six months following the treatment and showed no sign of recurrent or residual illness over a period of three years.
The tolerance to the drug and irradiation was perfect, that is, without major phototoxic incident causing prolonged gaps in the treatment.
Localized actinic erythemas, which were rapidly regressive, appeared on some patients who had a high sensitivity.
It should be mentioned in this regard that the patients thus treated and for whom the treatment was totally successful generally had type I skin.
Type I skin is particularly prone to skin cancers and notably to phototoxic incidents.
In other clinical trials on the same types of epidermic proliferation tumours, the treatment consisted in a topical administration of 5methoxypsoralene in concentrations of 1,000 to 10,000 ppm, which was then doubled by an oral administration of tablets containing 5methoxypsoralene and UV.A exposure with an average energy of 5 joules/cm2. Once again the results were spectacular and there was total necrosis of the cancerous cells.
The daily posology for the oral treatment of the cancerous tumours may be as much as 400 to 800 mg of 5-methoxypsoralene due to the low toxicity of the latter. It is preferable to increase the dose of active substance rather than the quantity of energy distributed so that the UV.A exposure should always remain within the range of 10 joules/cm2.
In the case of malignant tumours of the mucous membranes accessible by the natural routes, treatment such as that described above is directly applicable, since UV.A radiation is able to penetrate to the very depth of the dermis. In the case of inner malignant tumours, the administration of 5-methoxypsoralene has to be followed by an exposure to a more penetrating radiation with an appropriate wave-length in order to bring the necessary energy to the deeper sites.

Claims (6)

1. Drugs for the treatment by the topical route of epidermic proliferation cancerous tumours, characterized in that they contain an active substance 5-methoxypsora lene at concentrations of 1,000 ppm to 10,000 ppm, in a therapeutically acceptable carrier.
2. Drugs according to claim 1, characterized in that they further contain penetration agents.
3. Drugs according to claim 2, wherein the penetration agent is dimethyl sulphoxide (DMSO).
4. Drugs according to claims 1 to 3, wherein the therapeutically acceptable carriers are petroleum jellies, mineral and vegetable oils, oily continuous phase emulsions, alcoholic solutions, etc.
5. Drugs for the treatment by the oral route of cancerous or pre-cancerous tumours, characterized in that they contain as active substance 5-methoxypsoralene in the form of tablets containing 200 to 400 mg of active substance per tablet.
6. Drugs according to any one of the preceding claims 1 to 5, characterized in that they are activated by UV.A exposure or by any other appropriate radiation.
GB08315070A 1982-04-09 1983-06-01 Drugs containing a psoralene derivative Expired GB2140686B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR8206262A FR2524801B1 (en) 1982-04-09 1982-04-09 DRUGS CONTAINING A PSORALENE DERIVATIVE
BE0/210731A BE896700A (en) 1982-04-09 1983-05-09 MEDICINAL PRODUCTS CONTAINING A PSORALENE DERIVATIVE.

Publications (3)

Publication Number Publication Date
GB8315070D0 GB8315070D0 (en) 1983-07-06
GB2140686A true GB2140686A (en) 1984-12-05
GB2140686B GB2140686B (en) 1986-09-17

Family

ID=36782343

Family Applications (1)

Application Number Title Priority Date Filing Date
GB08315070A Expired GB2140686B (en) 1982-04-09 1983-06-01 Drugs containing a psoralene derivative

Country Status (7)

Country Link
JP (1) JPH0653664B2 (en)
AU (1) AU559029B2 (en)
BE (1) BE896700A (en)
CA (1) CA1205386A (en)
CH (1) CH656801A5 (en)
FR (1) FR2524801B1 (en)
GB (1) GB2140686B (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0756477A4 (en) * 1994-03-15 1999-05-19 Gen Hospital Corp METHODS OF PHOTOTHERAPEUTIC TREATMENT OF PROLIFERATIVE SKIN DISEASES

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9106365D0 (en) * 1991-03-26 1991-05-15 Bioglan Lab Ltd An emollient for use with ultraviolet light
FR2695036B1 (en) * 1992-09-03 1994-10-28 Goupil Jean Jacques Oil containing 5-methoxypsoralen at a concentration of 60 to 100 PPM and its use for the treatment of psoriasis.
CN116102713A (en) * 2022-09-07 2023-05-12 江苏三木化工股份有限公司 A kind of multi-arm structure amine epoxy curing agent and preparation method thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2406444A1 (en) * 1977-10-21 1979-05-18 Goupil Jean Jacques 5-Methoxy-psoralen for psoriasis treatment - prepd. from phloroglucinol via mono-methyl ether, 6-hydroxy-4-methoxy-coumaran-3-one and coumaran
LU80347A1 (en) * 1977-10-21 1979-03-16 Goupil J 5-METHOXY-PSORALENE AS A NEW MEDICINAL PRODUCT AND SYNTHESIS

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0756477A4 (en) * 1994-03-15 1999-05-19 Gen Hospital Corp METHODS OF PHOTOTHERAPEUTIC TREATMENT OF PROLIFERATIVE SKIN DISEASES

Also Published As

Publication number Publication date
AU1490583A (en) 1984-11-29
JPH0653664B2 (en) 1994-07-20
JPS59222413A (en) 1984-12-14
GB8315070D0 (en) 1983-07-06
AU559029B2 (en) 1987-02-19
FR2524801B1 (en) 1985-08-30
CA1205386A (en) 1986-06-03
FR2524801A1 (en) 1983-10-14
CH656801A5 (en) 1986-07-31
BE896700A (en) 1983-09-01
GB2140686B (en) 1986-09-17

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Date Code Title Description
PCNP Patent ceased through non-payment of renewal fee

Effective date: 19960601