CN110891575A - 治疗和/或预防光化性角化病的方法 - Google Patents
治疗和/或预防光化性角化病的方法 Download PDFInfo
- Publication number
- CN110891575A CN110891575A CN201880029861.9A CN201880029861A CN110891575A CN 110891575 A CN110891575 A CN 110891575A CN 201880029861 A CN201880029861 A CN 201880029861A CN 110891575 A CN110891575 A CN 110891575A
- Authority
- CN
- China
- Prior art keywords
- days
- subject
- administered
- day
- area
- 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.)
- Pending
Links
- 238000000034 method Methods 0.000 title claims abstract description 168
- 208000009621 actinic keratosis Diseases 0.000 title claims abstract description 142
- 238000011282 treatment Methods 0.000 claims description 156
- 230000000694 effects Effects 0.000 claims description 35
- 206010040914 Skin reaction Diseases 0.000 claims description 33
- 210000004761 scalp Anatomy 0.000 claims description 31
- 230000035483 skin reaction Effects 0.000 claims description 28
- 231100000430 skin reaction Toxicity 0.000 claims description 28
- 230000000699 topical effect Effects 0.000 claims description 26
- 230000002411 adverse Effects 0.000 claims description 24
- 230000002354 daily effect Effects 0.000 claims description 24
- 210000000245 forearm Anatomy 0.000 claims description 20
- 230000008961 swelling Effects 0.000 claims description 13
- 230000003810 hyperpigmentation Effects 0.000 claims description 12
- 208000000069 hyperpigmentation Diseases 0.000 claims description 11
- 206010037888 Rash pustular Diseases 0.000 claims description 10
- 208000029561 pustule Diseases 0.000 claims description 10
- 208000003367 Hypopigmentation Diseases 0.000 claims description 9
- 208000003251 Pruritus Diseases 0.000 claims description 9
- 208000025865 Ulcer Diseases 0.000 claims description 9
- 230000003628 erosive effect Effects 0.000 claims description 9
- 210000001508 eye Anatomy 0.000 claims description 9
- 210000001061 forehead Anatomy 0.000 claims description 9
- 210000004247 hand Anatomy 0.000 claims description 9
- 230000003425 hypopigmentation Effects 0.000 claims description 9
- 230000015572 biosynthetic process Effects 0.000 claims description 8
- 230000002265 prevention Effects 0.000 claims description 8
- 230000036269 ulceration Effects 0.000 claims description 8
- 230000007332 vesicle formation Effects 0.000 claims description 8
- 206010019233 Headaches Diseases 0.000 claims description 7
- 231100000869 headache Toxicity 0.000 claims description 7
- 210000002414 leg Anatomy 0.000 claims description 7
- 210000000088 lip Anatomy 0.000 claims description 7
- 210000005010 torso Anatomy 0.000 claims description 7
- 206010003051 Application site pain Diseases 0.000 claims description 6
- 208000002193 Pain Diseases 0.000 claims description 6
- 210000000617 arm Anatomy 0.000 claims description 6
- 210000005069 ears Anatomy 0.000 claims description 6
- 210000003739 neck Anatomy 0.000 claims description 6
- 210000001331 nose Anatomy 0.000 claims description 6
- 230000003442 weekly effect Effects 0.000 claims description 6
- 206010030113 Oedema Diseases 0.000 claims description 5
- 206010068319 Oropharyngeal pain Diseases 0.000 claims description 5
- 210000000744 eyelid Anatomy 0.000 claims description 5
- 210000002683 foot Anatomy 0.000 claims description 5
- 230000007803 itching Effects 0.000 claims description 5
- 201000009240 nasopharyngitis Diseases 0.000 claims description 5
- 230000036407 pain Effects 0.000 claims description 5
- 201000003004 ptosis Diseases 0.000 claims description 5
- 206010049041 Application site infection Diseases 0.000 claims description 3
- 206010003046 Application site irritation Diseases 0.000 claims description 3
- 206010003053 Application site pruritus Diseases 0.000 claims description 3
- 206010053424 Application site swelling Diseases 0.000 claims description 3
- 208000015181 infectious disease Diseases 0.000 claims description 3
- 230000007794 irritation Effects 0.000 claims description 3
- 206010006784 Burning sensation Diseases 0.000 claims description 2
- 230000035807 sensation Effects 0.000 claims description 2
- 208000023409 throat pain Diseases 0.000 claims 2
- 230000003203 everyday effect Effects 0.000 claims 1
- 230000003902 lesion Effects 0.000 description 77
- 239000003814 drug Substances 0.000 description 22
- VDJHFHXMUKFKET-UHFFFAOYSA-N Ingenol mebutate Natural products CC1CC2C(C)(C)C2C2C=C(CO)C(O)C3(O)C(OC(=O)C(C)=CC)C(C)=CC31C2=O VDJHFHXMUKFKET-UHFFFAOYSA-N 0.000 description 18
- 229940079593 drug Drugs 0.000 description 18
- VDJHFHXMUKFKET-WDUFCVPESA-N ingenol mebutate Chemical compound C[C@@H]1C[C@H]2C(C)(C)[C@H]2[C@@H]2C=C(CO)[C@@H](O)[C@]3(O)[C@@H](OC(=O)C(\C)=C/C)C(C)=C[C@]31C2=O VDJHFHXMUKFKET-WDUFCVPESA-N 0.000 description 18
- 229940107670 picato Drugs 0.000 description 18
- 206010015150 Erythema Diseases 0.000 description 12
- 206010042674 Swelling Diseases 0.000 description 10
- 238000002560 therapeutic procedure Methods 0.000 description 10
- 230000037390 scarring Effects 0.000 description 9
- 238000012216 screening Methods 0.000 description 9
- 239000002131 composite material Substances 0.000 description 8
- 231100000321 erythema Toxicity 0.000 description 8
- 210000002381 plasma Anatomy 0.000 description 8
- 230000036470 plasma concentration Effects 0.000 description 8
- 206010041823 squamous cell carcinoma Diseases 0.000 description 8
- VEBVPUXQAPLADL-UHFFFAOYSA-N Ingenol Natural products C1=C(CO)C(O)C2(O)C(O)C(C)=CC32C(C)CC2C(C)(C)C2C1C3=O VEBVPUXQAPLADL-UHFFFAOYSA-N 0.000 description 7
- VEBVPUXQAPLADL-POYOOMFHSA-N ingenol Chemical compound C1=C(CO)[C@@H](O)[C@]2(O)[C@@H](O)C(C)=C[C@]32[C@H](C)C[C@H]2C(C)(C)[C@H]2[C@H]1C3=O VEBVPUXQAPLADL-POYOOMFHSA-N 0.000 description 7
- 238000011200 topical administration Methods 0.000 description 7
- 206010004146 Basal cell carcinoma Diseases 0.000 description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
- 238000011156 evaluation Methods 0.000 description 6
- 239000000499 gel Substances 0.000 description 6
- 230000036961 partial effect Effects 0.000 description 6
- 208000024891 symptom Diseases 0.000 description 6
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 description 5
- 206010040844 Skin exfoliation Diseases 0.000 description 5
- 238000004458 analytical method Methods 0.000 description 5
- 230000003247 decreasing effect Effects 0.000 description 5
- 230000035618 desquamation Effects 0.000 description 5
- 229960002949 fluorouracil Drugs 0.000 description 5
- 230000009467 reduction Effects 0.000 description 5
- 230000004044 response Effects 0.000 description 5
- 230000006641 stabilisation Effects 0.000 description 5
- 238000011105 stabilization Methods 0.000 description 5
- 230000009885 systemic effect Effects 0.000 description 5
- CERQOIWHTDAKMF-UHFFFAOYSA-M Methacrylate Chemical compound CC(=C)C([O-])=O CERQOIWHTDAKMF-UHFFFAOYSA-M 0.000 description 4
- 208000000453 Skin Neoplasms Diseases 0.000 description 4
- 238000000315 cryotherapy Methods 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- 238000002428 photodynamic therapy Methods 0.000 description 4
- 201000000849 skin cancer Diseases 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 description 3
- 241000282414 Homo sapiens Species 0.000 description 3
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 3
- 201000007100 Pharyngitis Diseases 0.000 description 3
- 208000004403 Prostatic Hyperplasia Diseases 0.000 description 3
- 206010059516 Skin toxicity Diseases 0.000 description 3
- 230000002159 abnormal effect Effects 0.000 description 3
- 238000010171 animal model Methods 0.000 description 3
- 238000001574 biopsy Methods 0.000 description 3
- 239000006071 cream Substances 0.000 description 3
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 description 3
- 229960001259 diclofenac Drugs 0.000 description 3
- 230000007717 exclusion Effects 0.000 description 3
- DOUYETYNHWVLEO-UHFFFAOYSA-N imiquimod Chemical compound C1=CC=CC2=C3N(CC(C)C)C=NC3=C(N)N=C21 DOUYETYNHWVLEO-UHFFFAOYSA-N 0.000 description 3
- 229960002751 imiquimod Drugs 0.000 description 3
- 238000002483 medication Methods 0.000 description 3
- MCVVUJPXSBQTRZ-ONEGZZNKSA-N methyl (e)-but-2-enoate Chemical compound COC(=O)\C=C\C MCVVUJPXSBQTRZ-ONEGZZNKSA-N 0.000 description 3
- 238000011002 quantification Methods 0.000 description 3
- 230000035945 sensitivity Effects 0.000 description 3
- 231100000438 skin toxicity Toxicity 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 238000011269 treatment regimen Methods 0.000 description 3
- 208000019750 Administration site reaction Diseases 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 206010015995 Eyelid ptosis Diseases 0.000 description 2
- 206010020649 Hyperkeratosis Diseases 0.000 description 2
- 102000014150 Interferons Human genes 0.000 description 2
- 108010050904 Interferons Proteins 0.000 description 2
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 description 2
- 206010028372 Muscular weakness Diseases 0.000 description 2
- 201000002481 Myositis Diseases 0.000 description 2
- 206010041101 Small intestinal obstruction Diseases 0.000 description 2
- 206010052428 Wound Diseases 0.000 description 2
- 238000009825 accumulation Methods 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 238000003556 assay Methods 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 238000002681 cryosurgery Methods 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 229940000406 drug candidate Drugs 0.000 description 2
- YMTINGFKWWXKFG-UHFFFAOYSA-N fenofibrate Chemical compound C1=CC(OC(C)(C)C(=O)OC(C)C)=CC=C1C(=O)C1=CC=C(Cl)C=C1 YMTINGFKWWXKFG-UHFFFAOYSA-N 0.000 description 2
- 229960002297 fenofibrate Drugs 0.000 description 2
- 210000003128 head Anatomy 0.000 description 2
- 230000036541 health Effects 0.000 description 2
- 230000001329 hyperkeratotic effect Effects 0.000 description 2
- 230000001969 hypertrophic effect Effects 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000009533 lab test Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 229960000485 methotrexate Drugs 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 239000002547 new drug Substances 0.000 description 2
- 210000000056 organ Anatomy 0.000 description 2
- 201000008482 osteoarthritis Diseases 0.000 description 2
- 238000013105 post hoc analysis Methods 0.000 description 2
- 238000009597 pregnancy test Methods 0.000 description 2
- 230000007115 recruitment Effects 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 238000012552 review Methods 0.000 description 2
- 150000003431 steroids Chemical class 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 231100000331 toxic Toxicity 0.000 description 2
- 230000002588 toxic effect Effects 0.000 description 2
- 238000002562 urinalysis Methods 0.000 description 2
- ZGXJTSGNIOSYLO-UHFFFAOYSA-N 88755TAZ87 Chemical compound NCC(=O)CCC(O)=O ZGXJTSGNIOSYLO-UHFFFAOYSA-N 0.000 description 1
- 206010056951 Actinic cheilitis Diseases 0.000 description 1
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 206010003055 Application site reaction Diseases 0.000 description 1
- 208000006820 Arthralgia Diseases 0.000 description 1
- 208000008035 Back Pain Diseases 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 description 1
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 description 1
- 108010036949 Cyclosporine Proteins 0.000 description 1
- 201000004624 Dermatitis Diseases 0.000 description 1
- 206010012438 Dermatitis atopic Diseases 0.000 description 1
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical class OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 208000031226 Hyperlipidaemia Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 206010062016 Immunosuppression Diseases 0.000 description 1
- SHGAZHPCJJPHSC-NUEINMDLSA-N Isotretinoin Chemical compound OC(=O)C=C(C)/C=C/C=C(C)C=CC1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-NUEINMDLSA-N 0.000 description 1
- 208000001126 Keratosis Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 208000010428 Muscle Weakness Diseases 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 206010057190 Respiratory tract infections Diseases 0.000 description 1
- 206010039580 Scar Diseases 0.000 description 1
- 206010040865 Skin hyperpigmentation Diseases 0.000 description 1
- 241000282887 Suidae Species 0.000 description 1
- NAVMQTYZDKMPEU-UHFFFAOYSA-N Targretin Chemical compound CC1=CC(C(CCC2(C)C)(C)C)=C2C=C1C(=C)C1=CC=C(C(O)=O)C=C1 NAVMQTYZDKMPEU-UHFFFAOYSA-N 0.000 description 1
- 102000003929 Transaminases Human genes 0.000 description 1
- 108090000340 Transaminases Proteins 0.000 description 1
- 206010046306 Upper respiratory tract infection Diseases 0.000 description 1
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 description 1
- 208000000260 Warts Diseases 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 229960005339 acitretin Drugs 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- IHUNBGSDBOWDMA-AQFIFDHZSA-N all-trans-acitretin Chemical compound COC1=CC(C)=C(\C=C\C(\C)=C\C=C\C(\C)=C\C(O)=O)C(C)=C1C IHUNBGSDBOWDMA-AQFIFDHZSA-N 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 150000001280 alpha hydroxy acids Chemical class 0.000 description 1
- 229960002749 aminolevulinic acid Drugs 0.000 description 1
- 230000003466 anti-cipated effect Effects 0.000 description 1
- 201000008937 atopic dermatitis Diseases 0.000 description 1
- 208000010668 atopic eczema Diseases 0.000 description 1
- 239000005667 attractant Substances 0.000 description 1
- 229960002170 azathioprine Drugs 0.000 description 1
- LMEKQMALGUDUQG-UHFFFAOYSA-N azathioprine Chemical compound CN1C=NC([N+]([O-])=O)=C1SC1=NC=NC2=C1NC=N2 LMEKQMALGUDUQG-UHFFFAOYSA-N 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 150000001277 beta hydroxy acids Chemical class 0.000 description 1
- 229960002938 bexarotene Drugs 0.000 description 1
- 230000002146 bilateral effect Effects 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- JCKYGMPEJWAADB-UHFFFAOYSA-N chlorambucil Chemical compound OC(=O)CCCC1=CC=C(N(CCCl)CCCl)C=C1 JCKYGMPEJWAADB-UHFFFAOYSA-N 0.000 description 1
- 229960004630 chlorambucil Drugs 0.000 description 1
- 229960001265 ciclosporin Drugs 0.000 description 1
- 229940124301 concurrent medication Drugs 0.000 description 1
- 239000003433 contraceptive agent Substances 0.000 description 1
- 229940124558 contraceptive agent Drugs 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- 238000012864 cross contamination Methods 0.000 description 1
- 229960004397 cyclophosphamide Drugs 0.000 description 1
- 229930182912 cyclosporin Natural products 0.000 description 1
- 231100000433 cytotoxic Toxicity 0.000 description 1
- 230000001472 cytotoxic effect Effects 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 231100000517 death Toxicity 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 239000000890 drug combination Substances 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 235000013601 eggs Nutrition 0.000 description 1
- 238000002565 electrocardiography Methods 0.000 description 1
- 230000001667 episodic effect Effects 0.000 description 1
- 210000003414 extremity Anatomy 0.000 description 1
- 230000035558 fertility Effects 0.000 description 1
- 239000012458 free base Substances 0.000 description 1
- 230000012010 growth Effects 0.000 description 1
- 230000003862 health status Effects 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 238000009802 hysterectomy Methods 0.000 description 1
- 210000000987 immune system Anatomy 0.000 description 1
- 239000002955 immunomodulating agent Substances 0.000 description 1
- 229940121354 immunomodulator Drugs 0.000 description 1
- 230000001506 immunosuppresive effect Effects 0.000 description 1
- 230000036512 infertility Effects 0.000 description 1
- 208000000509 infertility Diseases 0.000 description 1
- 231100000535 infertility Toxicity 0.000 description 1
- 229960000598 infliximab Drugs 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 229940079322 interferon Drugs 0.000 description 1
- 229940047124 interferons Drugs 0.000 description 1
- 229960005280 isotretinoin Drugs 0.000 description 1
- 231100000518 lethal Toxicity 0.000 description 1
- 230000001665 lethal effect Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000001294 liquid chromatography-tandem mass spectrometry Methods 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 239000003550 marker Substances 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 230000005906 menstruation Effects 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 208000011873 mild conjunctivitis Diseases 0.000 description 1
- 210000003097 mucus Anatomy 0.000 description 1
- 230000036473 myasthenia Effects 0.000 description 1
- 208000031225 myocardial ischemia Diseases 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 231100001079 no serious adverse effect Toxicity 0.000 description 1
- 231100001099 no skin toxicity Toxicity 0.000 description 1
- 231100000344 non-irritating Toxicity 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 238000009806 oophorectomy Methods 0.000 description 1
- 239000000697 oral hormonal contraceptive Substances 0.000 description 1
- 230000027758 ovulation cycle Effects 0.000 description 1
- 210000003800 pharynx Anatomy 0.000 description 1
- 210000004623 platelet-rich plasma Anatomy 0.000 description 1
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 description 1
- 229960004618 prednisone Drugs 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 208000037922 refractory disease Diseases 0.000 description 1
- 238000002271 resection Methods 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- -1 salt compound Chemical class 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 201000010153 skin papilloma Diseases 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 231100001274 therapeutic index Toxicity 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 238000009810 tubal ligation Methods 0.000 description 1
- 231100000397 ulcer Toxicity 0.000 description 1
- 208000019206 urinary tract infection Diseases 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 238000007879 vasectomy Methods 0.000 description 1
- 229960003048 vinblastine Drugs 0.000 description 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
Images
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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
Landscapes
- 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)
- Dermatology (AREA)
- Epidemiology (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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762469889P | 2017-03-10 | 2017-03-10 | |
| US62/469,889 | 2017-03-10 | ||
| PCT/US2018/021929 WO2018165647A1 (en) | 2017-03-10 | 2018-03-12 | Methods of treating and/or preventing actinic keratosis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110891575A true CN110891575A (zh) | 2020-03-17 |
Family
ID=63446658
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880029861.9A Pending CN110891575A (zh) | 2017-03-10 | 2018-03-12 | 治疗和/或预防光化性角化病的方法 |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US10617693B2 (https=) |
| EP (2) | EP3592355B1 (https=) |
| JP (3) | JP7502863B2 (https=) |
| KR (2) | KR20240090837A (https=) |
| CN (1) | CN110891575A (https=) |
| AU (2) | AU2018231144B2 (https=) |
| BR (1) | BR112019018687A2 (https=) |
| CA (1) | CA3055938A1 (https=) |
| DK (1) | DK3592355T3 (https=) |
| ES (1) | ES3060528T3 (https=) |
| FI (1) | FI3592355T3 (https=) |
| HR (1) | HRP20260155T1 (https=) |
| IL (1) | IL269182B2 (https=) |
| LT (1) | LT3592355T (https=) |
| MX (2) | MX387658B (https=) |
| NZ (1) | NZ757105A (https=) |
| PL (1) | PL3592355T3 (https=) |
| PT (1) | PT3592355T (https=) |
| RS (1) | RS67713B1 (https=) |
| SI (1) | SI3592355T1 (https=) |
| TW (1) | TWI841523B (https=) |
| WO (1) | WO2018165647A1 (https=) |
| ZA (1) | ZA202100106B (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2025077886A1 (zh) * | 2023-10-13 | 2025-04-17 | 恩康药业科技（广州）有限公司 | 治疗和/或预防日光性角化病的化合物及方法 |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7968574B2 (en) * | 2004-12-28 | 2011-06-28 | Kinex Pharmaceuticals, Llc | Biaryl compositions and methods for modulating a kinase cascade |
| FI3592355T3 (fi) * | 2017-03-10 | 2026-02-13 | Atnx Spv Llc | KX2-391/KX-01 käytettäväksi aktiinisen keratoosin hoidossa |
| IL326637A (en) | 2017-09-07 | 2026-04-01 | Atnx Spv Llc | Solid forms of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide |
| CN117599189A (zh) * | 2018-03-07 | 2024-02-27 | 慧源Spv公司 | 用于治疗过度增殖性皮肤障碍的组合物和方法 |
| JP7296945B2 (ja) * | 2018-03-28 | 2023-06-23 | テルモ株式会社 | 医療デバイス |
| WO2020247706A1 (en) * | 2019-06-05 | 2020-12-10 | Athenex, Inc. | Methods of treating and/or preventing psoriasis |
| JP2024506240A (ja) * | 2021-01-21 | 2024-02-13 | サーナオミクス インコーポレイテッド | 皮膚がんの治療のための組成物および方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110021555A1 (en) * | 2008-12-19 | 2011-01-27 | Graceway Pharmaceuticals, Llc | Lower dosage strength imiquimod formulations and shorter dosing regimens for treating actinic keratoses |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7968574B2 (en) | 2004-12-28 | 2011-06-28 | Kinex Pharmaceuticals, Llc | Biaryl compositions and methods for modulating a kinase cascade |
| ES2382068T3 (es) | 2004-12-28 | 2012-06-05 | Kinex Pharmaceuticals, Llc | Composiciones y métodos para tratar trastornos de proliferación celular |
| JP5564251B2 (ja) | 2006-06-29 | 2014-07-30 | キネックス ファーマシューティカルズ， エルエルシー | キナーゼカスケードを調節するためのビアリール組成物および方法 |
| WO2008030892A2 (en) | 2006-09-05 | 2008-03-13 | Bipar Sciences, Inc. | Drug design for tubulin inhibitors, compositions, and methods of treatment thereof |
| US7939529B2 (en) | 2007-05-17 | 2011-05-10 | Kinex Pharmaceuticals, Llc | Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof |
| US7935697B2 (en) * | 2006-12-28 | 2011-05-03 | Kinex Pharmaceuticals, Llc | Compositions for modulating a kinase cascade and methods of use thereof |
| TWI457336B (zh) | 2006-12-28 | 2014-10-21 | Kinex Pharmaceuticals Llc | 調節激酶級聯之組成物及方法 |
| WO2008144045A1 (en) | 2007-05-17 | 2008-11-27 | Kinex Pharmaceuticals, Llc | Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof |
| EP2143421A1 (en) | 2008-07-07 | 2010-01-13 | Almirall Hermal GmbH | Topical composition for the treatment of actinic keratosis |
| NZ606177A (en) * | 2012-01-30 | 2014-03-28 | Dolorgiet Gmbh & Co Kg | Compositions for the treatment of actinic keratosis |
| US8741857B1 (en) * | 2012-01-30 | 2014-06-03 | Lawrence Moy | Treatments for actinic keratoses |
| JP6280546B2 (ja) | 2012-06-26 | 2018-02-14 | デル マー ファーマシューティカルズ | ジアンヒドロガラクチトール、ジアセチルジアンヒドロガラクチトール、ジブロモズルシトール、又はこれらの類似体若しくは誘導体を用いた、遺伝子多型又はａｈｉ１の調節不全若しくは変異を有する患者におけるチロシンキナーゼインヒビター抵抗性悪性腫瘍を処置するための方法 |
| FI3592355T3 (fi) * | 2017-03-10 | 2026-02-13 | Atnx Spv Llc | KX2-391/KX-01 käytettäväksi aktiinisen keratoosin hoidossa |
-
2018
- 2018-03-12 FI FIEP18764980.1T patent/FI3592355T3/fi active
- 2018-03-12 RS RS20260134A patent/RS67713B1/sr unknown
- 2018-03-12 CA CA3055938A patent/CA3055938A1/en active Pending
- 2018-03-12 IL IL269182A patent/IL269182B2/en unknown
- 2018-03-12 BR BR112019018687-5A patent/BR112019018687A2/pt not_active Application Discontinuation
- 2018-03-12 SI SI201831294T patent/SI3592355T1/sl unknown
- 2018-03-12 DK DK18764980.1T patent/DK3592355T3/da active
- 2018-03-12 EP EP18764980.1A patent/EP3592355B1/en active Active
- 2018-03-12 PT PT187649801T patent/PT3592355T/pt unknown
- 2018-03-12 ES ES18764980T patent/ES3060528T3/es active Active
- 2018-03-12 US US15/918,100 patent/US10617693B2/en active Active
- 2018-03-12 AU AU2018231144A patent/AU2018231144B2/en active Active
- 2018-03-12 EP EP25210508.5A patent/EP4659740A3/en active Pending
- 2018-03-12 MX MX2019010707A patent/MX387658B/es unknown
- 2018-03-12 JP JP2019549396A patent/JP7502863B2/ja active Active
- 2018-03-12 KR KR1020247017149A patent/KR20240090837A/ko active Pending
- 2018-03-12 LT LTEPPCT/US2018/021929T patent/LT3592355T/lt unknown
- 2018-03-12 TW TW107108242A patent/TWI841523B/zh active
- 2018-03-12 CN CN201880029861.9A patent/CN110891575A/zh active Pending
- 2018-03-12 PL PL18764980.1T patent/PL3592355T3/pl unknown
- 2018-03-12 HR HRP20260155TT patent/HRP20260155T1/hr unknown
- 2018-03-12 NZ NZ757105A patent/NZ757105A/en unknown
- 2018-03-12 WO PCT/US2018/021929 patent/WO2018165647A1/en not_active Ceased
- 2018-03-12 KR KR1020197029678A patent/KR20190141661A/ko not_active Ceased
-
2019
- 2019-09-09 MX MX2021013354A patent/MX2021013354A/es unknown
-
2020
- 2020-02-28 US US16/804,092 patent/US11497750B2/en active Active
-
2021
- 2021-01-07 ZA ZA2021/00106A patent/ZA202100106B/en unknown
-
2022
- 2022-10-11 US US17/963,502 patent/US20230172942A1/en active Pending
- 2022-11-11 JP JP2022180723A patent/JP2023015269A/ja active Pending
-
2024
- 2024-03-20 AU AU2024201828A patent/AU2024201828B2/en active Active
- 2024-11-28 JP JP2024207319A patent/JP2025029010A/ja active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110021555A1 (en) * | 2008-12-19 | 2011-01-27 | Graceway Pharmaceuticals, Llc | Lower dosage strength imiquimod formulations and shorter dosing regimens for treating actinic keratoses |
Non-Patent Citations (2)
| Title |
|---|
| KINEX PHARMACEUTICALS: "Kinex Pharmaceuticals Announces Allowance of the Investigational New Drug (IND) application for KX2-391 Ointment by the United States Food and Drug Administration (FDA)", 《HTTPS://WWW.PRNEWSWIRE.COM/NEWS- RELEASES/KINEX-PHARMACEUTICALS-ANNOUNCES-ALLOWANCE-OF-THE-INVESTIGATIONAL-NEW-DRUG-IND-APPLICATION-FOR-KX2-391-OINTMENT-BY-THE-UNITED-STATES-FOOD-AND-DRUG-ADMINISTRATION-FDA-268466522.HTML》 * |
| 赵文丽: "FDA 接受 KX2-391 软膏治疗光化性角化病的研究性新药申请", 《国际药学研究杂志》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2025077886A1 (zh) * | 2023-10-13 | 2025-04-17 | 恩康药业科技（广州）有限公司 | 治疗和/或预防日光性角化病的化合物及方法 |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2024201828B2 (en) | Methods of treating and/or preventing actinic keratosis | |
| CN105792829A (zh) | 使用伊维菌素治疗丘疹脓疱性红斑痤疮 | |
| US9713608B2 (en) | Method for topically treating actinic keratosis on the trunk (except chest) or extremities with ingenol 3-(3,5-diethylisoxazole-4-carboxylate) | |
| RU2805929C2 (ru) | Способы лечения и/или предотвращения актинического кератоза | |
| HK40020549A (en) | Kx2‑391/kx‑01 for use in the treatment of actinic keratosis | |
| HK40020549B (en) | Kx2‑391/kx‑01 for use in the treatment of actinic keratosis | |
| Mokadem et al. | Intralesional methotrexate versus curettage and application of 100% trichloroacetic acid in planter warts | |
| BR122025000862A2 (pt) | Usos do composto kx-01 no tratamento e/ou prevenção da ceratose actínica | |
| TW202112379A (zh) | 治療及／或預防乾癬之方法 | |
| Abbas et al. | The role of antimetabolite medication compared with traditional technique (cryotherapy) for treatment of verrucae | |
| TWI418347B (zh) | 治療疱疹病毒感染的方法 | |
| Dermotoi | Therapeutics 45 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB03 | Change of inventor or designer information | ||
| CB03 | Change of inventor or designer information |
Inventor after: Guan Mianfen Inventor after: Liu Yaonan Inventor after: E. D. Kramer Inventor after: D.L. Cutler Inventor after: Fang Rongsheng Inventor before: M-F.R.Guan Inventor before: J.Y-N.Liu Inventor before: E. D. Kramer Inventor before: D.L. Cutler Inventor before: J.Fang |
|
| TA01 | Transfer of patent application right | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20230413 Address after: New York, United States Applicant after: Anzix Special Purpose Co.,Ltd. Address before: New York, United States Applicant before: Abbott |