WO2016077648A1 - Méthode de traitement d'une lésion pré-cancéreuse avec du glyphosate, et compositions correspondantes - Google Patents

Méthode de traitement d'une lésion pré-cancéreuse avec du glyphosate, et compositions correspondantes Download PDF

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Publication number
WO2016077648A1
WO2016077648A1 PCT/US2015/060482 US2015060482W WO2016077648A1 WO 2016077648 A1 WO2016077648 A1 WO 2016077648A1 US 2015060482 W US2015060482 W US 2015060482W WO 2016077648 A1 WO2016077648 A1 WO 2016077648A1
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WO
WIPO (PCT)
Prior art keywords
lesion
composition
giyphosate
daim
skin
Prior art date
Application number
PCT/US2015/060482
Other languages
English (en)
Inventor
Calvin E. NEYMEYER
Original Assignee
Neymeyer Calvin E
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Neymeyer Calvin E filed Critical Neymeyer Calvin E
Publication of WO2016077648A1 publication Critical patent/WO2016077648A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like

Definitions

  • This invention is directed to th3 ⁇ 4 use of gjyphosate compositions to treat pre-tancerous skin lesions.
  • Skirt cancer Is a com n form of carscer, with thousands of people diagnosed and dying from it every year. Pre-cancerous lesions such as actinic keratosis may precede the formation and diagnosis of cancer of the skies, and cause discomfort arid other problems,
  • Giyphosate is an effective bnt controversial herbicide, with environmentalist and other groups concerned in part with mild to moderate systemic end dermal toxicity reported from contact with glyphosate-contaifiing compositions.
  • a safe, efficacious treatment for pre-cancerous lesions would be beneficial.
  • the present invention is directed to the use of giyphosate-contaioing compositions in the treatment of pre-cancerous skin lessens.
  • a glyphosate composition is administered by directly, topically applying the composition to a lesion. The lessors disappears and appears to be fully cored within weeks or evers days, such that th skin regains the appearance of adjacent, healthy skin,
  • the present invention is also directed to a composition comprising gfyphosate for the treatment of pre-cancerous skin lesions; and to the ose of a composition comprising glyphosate, for the preparation of a medicament for the treatment of a pre-cancerous skin lessors,
  • the present invention is directed to a method for treating a pre-cancerous lessors with glyphosata, comprising the step of topically applying the glyphosata to the lesion in s therapeutically effective amount
  • the present invention is also directed to a composition comprising glyphosate for instance as discussed above, for the treatment of a pre-cancerous sksn lesion. Also, the present invention is directed to the use of s composition comprising glyphosate of the present invention, for the preparation of a medicament for the treatment of a pre-cancerous skin lesion.
  • ski cancer refers to any type of cancer of the skin including for instance melanoma, basal cell cancer, or squamous ceil cancer
  • a "pre-carscersus lesson” refers to a change in the skin that is not yet cancerous but may become so, including for instance an actinic keratosis.
  • a pre-caneerous lesion is a small reddeoed raised area that may have a small scab, as described in the Examples.
  • Topical refers to the external surface of the skin
  • a composition having giyphosate is administered according to the present invention through topical application of the composition to a pre-cancerous lesion; piecing the composition in direct con act with ths lesion
  • Topical application can include a variety of known methods, including by drop, by application via finger, or for instance a cotton pad.
  • the composition is applied to an abraded lesion with gentle rubbing.
  • treat refers to ameliorating (improving or making less severe ⁇ end/or preferably to coring a pre-cancerous lesion.
  • Said treatment may occur in a human or non-homan subject having a pre-caneerous lesion.
  • a precancerous lesion treated according to the present invention is folly cured, and tha skin healed.
  • Treatment according to the present invention may be achieved by applying a composition of the present invention one or more times to the pre-canceroos lesion.
  • the composition is applied et feast two, and more preferably at least three, times during a course of treatment.
  • the composition is applied fewer than 20 times, more preferably fewer than 10 times, more preferably fewsr than 5 times, and most preferably 3 times, 2 times, or 1 time during the treatment of a given lesion or cancer, Multiple applications are preferably spaced 3 days to 14 days apart.
  • the composition of the present invention may be applied for instance 3 times, for instance one time every three days; or one time alone; or two times, for instance one week apart.
  • Other treatment schedules are also contemplated with regard to this invention, While the preferred treatment is a fuil cure, a composition of this invention may be applied for maintenance or preventative purposes.
  • compositions having a higher concentration of giyphosate may be used to provide a leading dose and a composition having a lower giyphosate eoneeotratioo f preferably approximately one-half of the composition used for the loading dose ⁇ for remaining applications.
  • terapéuticaally effective amount refers to an amount of giyphosate ⁇ 2 ⁇
  • giyphosate to a pre-cancerous lesion will include about 1 rng to about 400 g giyphosate; more preferably, about 4 mg to about 100 mg; more preferably, about 3 mg to about 90 mg; more preferably, about 4 mg to about 75 mg; more preferably, about 5 mg to ebout 30 mg; most preferably, about 5 to about 30 mg
  • Amounts applied to a precancerous lesion may be for instance 1, 2, 3, 4, S, 0, 7, S, 9, 10, 11-20, 21-30, 31-40, 41-50 f 51-60, 61-70, 71-80, 82-90, 91-100, 01-110, 111-120, 121-130, 31-140, 141-150, 52-1S0, 261-170, 171-180, 2
  • the giyphosate may be present in an amount of about 2% to about 99% of the composition.
  • the giyphosate may comprise for instance 1-5% giyphosate; 0-20% giyphosate; 11-15% giyphosate; 16-20% giyphosate; 21-25% giyphosate; 26-30% giyphosate; 31-35% giyphosate; 36-40% giyphosate; 41-45% giyphosate; 46-50% giyphosate; Si ⁇ S5% giyphosate; 56-60% giyphosate; 61-65% giyphosate; 86-70% giyphosate; 71-75% giyphosate; 76-80% giyphosate; S1-SS% giyphosate; ⁇ 5-90% giyphosate; S1-9S% gi
  • the giyphosate may also e pressnt in amount of about 1, 2, 3 f 4, 5, 6 f 7, 8, 9, 20, 11, 12, 23, 14, 15, 16, 17, 18, 19, 29, 21, 22, 23, 24, 25, 26, 27, 28, 2 ⁇ , 30, 31, 32, 33, 34, 35, 3S, 37, 36, 39, 40, 41, 42, 43, 44, 45, 46, 7, 8, 49, 50, 51, 52, 53, 54, 55, 55, 57, 58, 58, 60, 61, 62, 63, 64, ⁇ 5, 66, 07, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 3, g4, 85, 86, 87, 86, 89, 90, , 92, 93, 94, 95, 96, 97, 8, 99% by weight of the total composition.
  • a range including the above amounts is also contemplated in the context of the present invention,
  • a composition of the present invention may include giyphosate alone, or with one or more active ingredients, preferably also use ul In treating precancerous lesions, and/or one or more inactive ingredients, for instance to provide effective delivery of the giyphosate.
  • active ingredients i clude for instance water and minor formulating ingredients, as well as other compounds suitable for topical application
  • the giyphosate is in the form of an isopropylamine salt.
  • the composition ma be a liquid solution, gel, cream, ointment, or other form suitable for topical application to the skin.
  • the composition is in aqueous solution, more preferably the composition has an acidic pH, even more preferably a pH in the range of about 3,5 to about 6, arsd more preferably, a pH in the range of 4-5,
  • composition employed in the following examples are products identified in EPA Reg Mo, 71995-29, (Roun up Weed & Grass Kliier Concentrated Plus) EPA Reg No. 71995-27 and/or EPA Reg ffo. 71995-27- 239 fOrfho Basic Solutions Weed & grass Kliier Ready o-Use ( spray bottle, 1J2% giyphosate f'Qrtho com osition" ⁇ .
  • the Sv SOS for these products are i clude herewith and incorporated by reference as needed to aid in describing compositions that may be used in the present invention.
  • a pre-cancersus lesion (actinic keratosis on an elderly man's face was treated with a giyphosate composition.
  • the lesion was small, approximately 1 mm in sits and located 20 mm to the left of the lower edge of the man's left nostril, The iasiors persisted for approximately 8 months prior to treatment according to the present invention, resisting three attempts at treatment with alcohol and/or topical antibiotics, stich that the lesion would redden slightly and trickle blood, but not heal
  • a small scab covered the lesion prior to treatment according to the present invention.
  • the scab, lesion, and area surrounding the lesion were gently cleansed with Dial liquid soap and the scab removed, to provide maximum ex osu e of the lesion to the giyphosate.
  • the lesion and surrounding area was observed dally, several times during the day, to follow the progression of the treated area, The redness began disappearing, and after four days, the skin was similar to surrounding tissue, although still with a slight difference.
  • the area was slightly reddish, blotchy, and there was a tiny erater where the lesion had been but appeared to be healing, no rawness, no scabbing, sod the skin appeared normal
  • the small lesson was treated and fully healed in 7 days, with Just one application of the Ortho composition.
  • a secorsd less n f actinic keratosis! on the same male subject was on the left side of the subject's throat, about SOmm directly below the subject's left ear. The leslofs would not heel. It would scab over for 3 to 4 days, and then the scab would leave, revealing the reddersed unhealed area underneath. The lesion was cove ed with antibiotics several times, causing it to scab and eventually slough off, again revealing a reddened unhealed area. The lesion was sensitive when touched; care was taken during shaving to avoid pain and worsening of the lesion. This continued for 6-8 months.
  • the second lesion was treated with the Ortho composition.
  • the lesion was thoroughly ciearssed with Dial li uid soap I ⁇ expose as much of the lesion as possible. Most of the lesion became exposed as the scab was gently removed. After cleaning, the lesion showed a raw, unhealed ares with a crater-like ap earance in the upper end of the unhealed area.
  • the lesson was not rubbed vigorously, but was rubbed firmly, to expose as much lesion tissue as possible.
  • the leslors was about IS mm long and gmm wide, running diagonally upward toward the left ear, with the top of the lesion about SOmm below the lobe of the left ear.
  • the Ortho composition was squirted mto the subject's hand and end of £Mip was immersed into the li uid, generally as discussed regarding the first lesion above. After gently s ueezing the esccess fluid from the Q-tip, the Ortho composition was topically applied to the lesion, so that the entire lesion was covered, with attempts to not x esid application much over the borders of the lesion.
  • the Ortho composition was directly end topically applied by gentle rubbing to a precancerous skin lesion (actinic keratosis) on the face of a human male subject, Just below his eye. Prior to treatment, the lesion was treated in the approximate manner described In Example I It is estimated that
  • Example ii The Ortho composition of Example ii was applied to a different lesion (ac inic keratosis) on the same sobject, having similar characteristics to that described in Example il . Applicatio occurred 3 times; Day 0, Day 3, and Day 7. It is estimated that each application included approximately 6.Q mg of glyphosate. The scab disappeared and redness and swelling lessened and then disappeared o1 ⁇ 43 ⁇ 4r the spars of the following 3 weeks. No adverse effects were reported by the subject.
  • a composition ⁇ EPA Reg. H. 71S95-2 ⁇ having approximately 1B% of iseprspylamine salt of glyphosate
  • pH about 5 was directly applied by gentle robbing to a pre-eancerous skin lesson (actinic keratosis! on the tip of the ear of a huma male subject, The lesion was small fabout 3 mm long and 2 mm wide) and scabbed, and was abraded prior to application of the composition to allow the composition direct access to the raw skin under the scab.
  • a blood blister appeared over the lesion and was punctured and drained during treatment.
  • the composition was reapplied 4 days after the initial application, with any scab again abraded.
  • the lesion was completely heeled within 10 days. Other than the formation of the blood blister, no adverse effects were reported by the subject.
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  • This product ss teidiius scsorfisa is i3 ⁇ 4e OSHA HSSSK ⁇ CofrmsKiseseien Sssadsrf.39 CFR S9I0.12C0.
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  • TLV (ACG!H): SJ m»3 ⁇ 43 ⁇ 43: faspiisfek fra ⁇ km. sk3 ⁇ 4, No s Kcjils ossstpasteijai «p «3 ⁇ 4f e lmis isss bse«i «3 ⁇ 4M:3 ⁇ 4«iJ v T3 ⁇ 4e es asw Uraii Mkaitd is for sha
  • f31 ⁇ 4ysM ⁇ dsis aire ij-pknf vakss feasesi m fjiatsriaS Jessed 3 ⁇ 4ssi msy vary ffcs scrapie ⁇ a snnspie.
  • Typical aStis* s ould soi be fcatssittiCiS as a gti aaiui'd iws!jsis s>f my specifst: to3 ⁇ 4 iir as ⁇ dikaiittns for i!sc fir& aa.
  • T&is ssct m h >.::: ⁇ . ⁇ >: ⁇ for sjja by iesiseS3 ⁇ 4isis ⁇ ⁇ 5 ofef health profssskmsk .
  • T is Is sfssSfjdcd fcr toe by ⁇ ? ⁇ ! ⁇ 5 ⁇ 3 ⁇ 4 ⁇ . «5 ssxi ti!hKf ewoliosss? spicjsikjs.

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une méthode de traitement d'une lésion pré-cancéreuse de la peau sur un sujet humain avec du glyphosate, ainsi que des compositions destinées à ce traitement.
PCT/US2015/060482 2014-11-11 2015-11-12 Méthode de traitement d'une lésion pré-cancéreuse avec du glyphosate, et compositions correspondantes WO2016077648A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462078403P 2014-11-11 2014-11-11
US62/078,403 2014-11-11

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Publication Number Publication Date
WO2016077648A1 true WO2016077648A1 (fr) 2016-05-19

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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6509325B1 (en) * 2000-05-02 2003-01-21 Albert Einstein College Of Medicine Of Yeshiva University Method for inhibiting melanogenesis and uses thereof
US20040077608A1 (en) * 2002-08-30 2004-04-22 Monsanto Technology Llc Glyphosate formulations and their use for the inhibition of 5-enolpyruvylshikimate-3-phosphate synthase
US20040254164A1 (en) * 2002-01-22 2004-12-16 Pfizer Inc. 3-(imidazolyl)-2-alkoxypropanoic acids
US20050192328A1 (en) * 1997-05-16 2005-09-01 Uaf Technologies And Research, Llc Compounds and methods for use thereof in the treatment of viral infections
US20100247463A1 (en) * 2006-01-10 2010-09-30 Yu Ruey J N-(phosphonoalkyl)-amino acids, derivatives thereof and compositions and methods of use
KR20130119912A (ko) * 2010-08-24 2013-11-01 지티엑스, 인코포레이티드 암 치료용 화합물

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050192328A1 (en) * 1997-05-16 2005-09-01 Uaf Technologies And Research, Llc Compounds and methods for use thereof in the treatment of viral infections
US6509325B1 (en) * 2000-05-02 2003-01-21 Albert Einstein College Of Medicine Of Yeshiva University Method for inhibiting melanogenesis and uses thereof
US20040254164A1 (en) * 2002-01-22 2004-12-16 Pfizer Inc. 3-(imidazolyl)-2-alkoxypropanoic acids
US20040077608A1 (en) * 2002-08-30 2004-04-22 Monsanto Technology Llc Glyphosate formulations and their use for the inhibition of 5-enolpyruvylshikimate-3-phosphate synthase
US20100247463A1 (en) * 2006-01-10 2010-09-30 Yu Ruey J N-(phosphonoalkyl)-amino acids, derivatives thereof and compositions and methods of use
KR20130119912A (ko) * 2010-08-24 2013-11-01 지티엑스, 인코포레이티드 암 치료용 화합물

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