CA3182431A1 - Methods and compositions for preventing and treating myopia with fingolimod, a sphingosine-1-phosphate receptor modulator, and derivatives thereof - Google Patents
Methods and compositions for preventing and treating myopia with fingolimod, a sphingosine-1-phosphate receptor modulator, and derivatives thereofInfo
- Publication number
- CA3182431A1 CA3182431A1 CA3182431A CA3182431A CA3182431A1 CA 3182431 A1 CA3182431 A1 CA 3182431A1 CA 3182431 A CA3182431 A CA 3182431A CA 3182431 A CA3182431 A CA 3182431A CA 3182431 A1 CA3182431 A1 CA 3182431A1
- Authority
- CA
- Canada
- Prior art keywords
- myopia
- subject
- composition
- years
- age
- 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
- 208000001491 myopia Diseases 0.000 title claims abstract description 117
- 230000004379 myopia Effects 0.000 title claims abstract description 110
- 239000000203 mixture Substances 0.000 title claims abstract description 66
- 238000000034 method Methods 0.000 title claims abstract description 40
- 229940075993 receptor modulator Drugs 0.000 title abstract description 30
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 title abstract description 25
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 title abstract description 25
- 229960000556 fingolimod Drugs 0.000 title description 10
- KKGQTZUTZRNORY-UHFFFAOYSA-N fingolimod Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 title description 10
- LRFKWQGGENFBFO-UHFFFAOYSA-N fingolimod phosphate Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)COP(O)(O)=O)C=C1 LRFKWQGGENFBFO-UHFFFAOYSA-N 0.000 claims abstract description 28
- 230000000694 effects Effects 0.000 claims description 18
- 239000003795 chemical substances by application Substances 0.000 claims description 17
- 238000009472 formulation Methods 0.000 claims description 13
- 239000003889 eye drop Substances 0.000 claims description 11
- 229940012356 eye drops Drugs 0.000 claims description 11
- 238000013266 extended drug release Methods 0.000 claims description 10
- 230000001629 suppression Effects 0.000 claims description 8
- 238000002347 injection Methods 0.000 claims description 3
- 239000007924 injection Substances 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 230000035515 penetration Effects 0.000 claims description 2
- 238000013265 extended release Methods 0.000 claims 1
- 208000022873 Ocular disease Diseases 0.000 abstract description 4
- 238000007910 systemic administration Methods 0.000 abstract description 3
- 230000009885 systemic effect Effects 0.000 abstract description 3
- 238000011200 topical administration Methods 0.000 abstract description 2
- 210000001508 eye Anatomy 0.000 description 50
- 210000000695 crystalline len Anatomy 0.000 description 47
- 239000003814 drug Substances 0.000 description 30
- 229940079593 drug Drugs 0.000 description 29
- PFWLFWPASULGAN-UHFFFAOYSA-N 7-methylxanthine Chemical compound N1C(=O)NC(=O)C2=C1N=CN2C PFWLFWPASULGAN-UHFFFAOYSA-N 0.000 description 24
- 238000011282 treatment Methods 0.000 description 24
- 230000004423 myopia development Effects 0.000 description 23
- 230000004515 progressive myopia Effects 0.000 description 22
- 229930003347 Atropine Natural products 0.000 description 21
- RKUNBYITZUJHSG-UHFFFAOYSA-N Hyosciamin-hydrochlorid Natural products CN1C(C2)CCC1CC2OC(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-UHFFFAOYSA-N 0.000 description 21
- RKUNBYITZUJHSG-SPUOUPEWSA-N atropine Chemical compound O([C@H]1C[C@H]2CC[C@@H](C1)N2C)C(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-SPUOUPEWSA-N 0.000 description 21
- 229960000396 atropine Drugs 0.000 description 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 21
- 201000010099 disease Diseases 0.000 description 20
- 150000001875 compounds Chemical class 0.000 description 18
- 239000008194 pharmaceutical composition Substances 0.000 description 16
- 108090000623 proteins and genes Proteins 0.000 description 14
- 230000003287 optical effect Effects 0.000 description 13
- 239000004480 active ingredient Substances 0.000 description 12
- 241000699670 Mus sp. Species 0.000 description 10
- 230000002068 genetic effect Effects 0.000 description 10
- 208000014733 refractive error Diseases 0.000 description 10
- 230000004353 induced myopia Effects 0.000 description 9
- 229910019142 PO4 Inorganic materials 0.000 description 8
- 238000012377 drug delivery Methods 0.000 description 8
- 239000010452 phosphate Substances 0.000 description 8
- 230000019491 signal transduction Effects 0.000 description 8
- 241000287828 Gallus gallus Species 0.000 description 6
- 235000013330 chicken meat Nutrition 0.000 description 6
- 230000002250 progressing effect Effects 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
- 208000024891 symptom Diseases 0.000 description 6
- 201000004569 Blindness Diseases 0.000 description 5
- 241000700198 Cavia Species 0.000 description 5
- 238000001647 drug administration Methods 0.000 description 5
- 230000007613 environmental effect Effects 0.000 description 5
- 230000012010 growth Effects 0.000 description 5
- 230000002974 pharmacogenomic effect Effects 0.000 description 5
- 230000002265 prevention Effects 0.000 description 5
- 210000001525 retina Anatomy 0.000 description 5
- 241001465754 Metazoa Species 0.000 description 4
- 239000013543 active substance Substances 0.000 description 4
- 230000004071 biological effect Effects 0.000 description 4
- 230000015556 catabolic process Effects 0.000 description 4
- 238000006731 degradation reaction Methods 0.000 description 4
- 238000011161 development Methods 0.000 description 4
- 230000018109 developmental process Effects 0.000 description 4
- 230000004438 eyesight Effects 0.000 description 4
- 238000011223 gene expression profiling Methods 0.000 description 4
- 230000000704 physical effect Effects 0.000 description 4
- 230000000007 visual effect Effects 0.000 description 4
- 241000282412 Homo Species 0.000 description 3
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 238000004458 analytical method Methods 0.000 description 3
- 238000013459 approach Methods 0.000 description 3
- 239000000872 buffer Substances 0.000 description 3
- 230000008859 change Effects 0.000 description 3
- 238000010276 construction Methods 0.000 description 3
- 238000009509 drug development Methods 0.000 description 3
- 230000004373 eye development Effects 0.000 description 3
- 230000014509 gene expression Effects 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 230000007774 longterm Effects 0.000 description 3
- 230000001575 pathological effect Effects 0.000 description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 3
- 230000004393 visual impairment Effects 0.000 description 3
- KIHYPELVXPAIDH-HNSNBQBZSA-N 1-[[4-[(e)-n-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-c-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid Chemical compound CCC1=CC(C(\C)=N\OCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 KIHYPELVXPAIDH-HNSNBQBZSA-N 0.000 description 2
- QDDQIPUKAXBMBX-UHFFFAOYSA-N 1-[[6-[(2-methoxy-4-propylphenyl)methoxy]-1-methyl-3,4-dihydronaphthalen-2-yl]methyl]azetidine-3-carboxylic acid Chemical compound COC1=CC(CCC)=CC=C1COC1=CC=C(C(C)=C(CN2CC(C2)C(O)=O)CC2)C2=C1 QDDQIPUKAXBMBX-UHFFFAOYSA-N 0.000 description 2
- XRVDGNKRPOAQTN-FQEVSTJZSA-N 5-[3-[(1s)-1-(2-hydroxyethylamino)-2,3-dihydro-1h-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxybenzonitrile Chemical compound C1=C(C#N)C(OC(C)C)=CC=C1C1=NC(C=2C=3CC[C@@H](C=3C=CC=2)NCCO)=NO1 XRVDGNKRPOAQTN-FQEVSTJZSA-N 0.000 description 2
- 208000002177 Cataract Diseases 0.000 description 2
- 241000282693 Cercopithecidae Species 0.000 description 2
- 208000010412 Glaucoma Diseases 0.000 description 2
- 208000024080 Myopic macular degeneration Diseases 0.000 description 2
- 241000288906 Primates Species 0.000 description 2
- 241000288754 Scandentia Species 0.000 description 2
- 241000251539 Vertebrata <Metazoa> Species 0.000 description 2
- 230000004308 accommodation Effects 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 230000002776 aggregation Effects 0.000 description 2
- 238000004220 aggregation Methods 0.000 description 2
- 229930013930 alkaloid Natural products 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 210000002159 anterior chamber Anatomy 0.000 description 2
- 238000000149 argon plasma sintering Methods 0.000 description 2
- LPAUOXUZGSBGDU-STDDISTJSA-N chembl1096146 Chemical compound O=C1N(C=2C(=CC=CC=2)C)C(=N/CCC)/S\C1=C/C1=CC=C(OC[C@H](O)CO)C(Cl)=C1 LPAUOXUZGSBGDU-STDDISTJSA-N 0.000 description 2
- 238000002144 chemical decomposition reaction Methods 0.000 description 2
- 238000011260 co-administration Methods 0.000 description 2
- 238000012937 correction Methods 0.000 description 2
- 230000001934 delay Effects 0.000 description 2
- 235000005911 diet Nutrition 0.000 description 2
- 230000037213 diet Effects 0.000 description 2
- 125000000524 functional group Chemical group 0.000 description 2
- 239000007903 gelatin capsule Substances 0.000 description 2
- 230000036541 health Effects 0.000 description 2
- 230000004402 high myopia Effects 0.000 description 2
- 230000007062 hydrolysis Effects 0.000 description 2
- 238000006460 hydrolysis reaction Methods 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 238000001294 liquid chromatography-tandem mass spectrometry Methods 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 238000010172 mouse model Methods 0.000 description 2
- 230000003647 oxidation Effects 0.000 description 2
- 238000007254 oxidation reaction Methods 0.000 description 2
- 229950008141 ozanimod Drugs 0.000 description 2
- 238000004806 packaging method and process Methods 0.000 description 2
- 230000037361 pathway Effects 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- RMHMFHUVIITRHF-UHFFFAOYSA-N pirenzepine Chemical compound C1CN(C)CCN1CC(=O)N1C2=NC=CC=C2NC(=O)C2=CC=CC=C21 RMHMFHUVIITRHF-UHFFFAOYSA-N 0.000 description 2
- 229960004633 pirenzepine Drugs 0.000 description 2
- 229940068196 placebo Drugs 0.000 description 2
- 239000000902 placebo Substances 0.000 description 2
- 229920005862 polyol Polymers 0.000 description 2
- 150000003077 polyols Chemical class 0.000 description 2
- 229950009275 ponesimod Drugs 0.000 description 2
- 238000001556 precipitation Methods 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 230000001739 rebound effect Effects 0.000 description 2
- 230000004044 response Effects 0.000 description 2
- 210000003786 sclera Anatomy 0.000 description 2
- 229950005693 siponimod Drugs 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 208000017803 syndromic myopia Diseases 0.000 description 2
- 239000006188 syrup Substances 0.000 description 2
- 235000020357 syrup Nutrition 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- YAPQBXQYLJRXSA-UHFFFAOYSA-N theobromine Chemical compound CN1C(=O)NC(=O)C2=C1N=CN2C YAPQBXQYLJRXSA-UHFFFAOYSA-N 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- UQGQAMARAMOEID-UHFFFAOYSA-N (3-aminocyclopentyl)-butylphosphinic acid Chemical compound CCCCP(O)(=O)C1CCC(N)C1 UQGQAMARAMOEID-UHFFFAOYSA-N 0.000 description 1
- XOESDNIUAWGCLU-UHFFFAOYSA-N 3-aminopropyl(cyclohexylmethyl)phosphinic acid Chemical compound NCCCP(O)(=O)CC1CCCCC1 XOESDNIUAWGCLU-UHFFFAOYSA-N 0.000 description 1
- 241000251468 Actinopterygii Species 0.000 description 1
- 241001465356 Atropa belladonna Species 0.000 description 1
- 208000033825 Chorioretinal atrophy Diseases 0.000 description 1
- GJSURZIOUXUGAL-UHFFFAOYSA-N Clonidine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NCCN1 GJSURZIOUXUGAL-UHFFFAOYSA-N 0.000 description 1
- 240000007154 Coffea arabica Species 0.000 description 1
- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- PANKHBYNKQNAHN-JTBLXSOISA-N Crocetin Natural products OC(=O)C(\C)=C/C=C/C(/C)=C\C=C\C=C(\C)/C=C/C=C(/C)C(O)=O PANKHBYNKQNAHN-JTBLXSOISA-N 0.000 description 1
- 235000004237 Crocus Nutrition 0.000 description 1
- 241000596148 Crocus Species 0.000 description 1
- 229940098778 Dopamine receptor agonist Drugs 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 102000056764 GABAA-rho receptor Human genes 0.000 description 1
- 108700010345 GABAA-rho receptor Proteins 0.000 description 1
- 244000111489 Gardenia augusta Species 0.000 description 1
- 235000018958 Gardenia augusta Nutrition 0.000 description 1
- INJOMKTZOLKMBF-UHFFFAOYSA-N Guanfacine Chemical compound NC(=N)NC(=O)CC1=C(Cl)C=CC=C1Cl INJOMKTZOLKMBF-UHFFFAOYSA-N 0.000 description 1
- FMPNFDSPHNUFOS-HQEQRHKESA-N Himbacine Natural products C(/[C@@H]1[C@H]2CCCC[C@@H]2C[C@@H]2C(=O)O[C@H]([C@H]12)C)=C\[C@@H]1CCC[C@H](C)N1C FMPNFDSPHNUFOS-HQEQRHKESA-N 0.000 description 1
- 206010020675 Hypermetropia Diseases 0.000 description 1
- 208000026350 Inborn Genetic disease Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 208000035967 Long Term Adverse Effects Diseases 0.000 description 1
- 241000282560 Macaca mulatta Species 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 description 1
- FMPNFDSPHNUFOS-UHFFFAOYSA-N N-Methyl-himandravin Natural products C12C(C)OC(=O)C2CC2CCCCC2C1C=CC1CCCC(C)N1C FMPNFDSPHNUFOS-UHFFFAOYSA-N 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 206010034960 Photophobia Diseases 0.000 description 1
- 208000002367 Retinal Perforations Diseases 0.000 description 1
- 206010038848 Retinal detachment Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 244000269722 Thea sinensis Species 0.000 description 1
- 244000299461 Theobroma cacao Species 0.000 description 1
- 235000005764 Theobroma cacao ssp. cacao Nutrition 0.000 description 1
- 235000005767 Theobroma cacao ssp. sphaerocarpum Nutrition 0.000 description 1
- 206010047513 Vision blurred Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000002350 accommodative effect Effects 0.000 description 1
- 229940121359 adenosine receptor antagonist Drugs 0.000 description 1
- 239000000048 adrenergic agonist Substances 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 150000003797 alkaloid derivatives Chemical class 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- VMWNQDUVQKEIOC-CYBMUJFWSA-N apomorphine Chemical compound C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 VMWNQDUVQKEIOC-CYBMUJFWSA-N 0.000 description 1
- 229960004046 apomorphine Drugs 0.000 description 1
- 230000004323 axial length Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000031018 biological processes and functions Effects 0.000 description 1
- 229960000074 biopharmaceutical Drugs 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 235000001046 cacaotero Nutrition 0.000 description 1
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical class CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 235000021466 carotenoid Nutrition 0.000 description 1
- PANKHBYNKQNAHN-JUMCEFIXSA-N carotenoid dicarboxylic acid Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C(=O)O)C=CC=C(/C)C(=O)O PANKHBYNKQNAHN-JUMCEFIXSA-N 0.000 description 1
- 150000001747 carotenoids Chemical class 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 229960002896 clonidine Drugs 0.000 description 1
- 229920001436 collagen Polymers 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 230000001276 controlling effect Effects 0.000 description 1
- PANKHBYNKQNAHN-MQQNZMFNSA-N crocetin Chemical compound OC(=O)C(/C)=C/C=C/C(/C)=C/C=C/C=C(\C)/C=C/C=C(\C)C(O)=O PANKHBYNKQNAHN-MQQNZMFNSA-N 0.000 description 1
- 239000000634 cycloplegic agent Substances 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 230000009274 differential gene expression Effects 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 239000003136 dopamine receptor stimulating agent Substances 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 229940000406 drug candidate Drugs 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 230000036040 emmetropia Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 230000002255 enzymatic effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 239000003925 fat Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 238000009459 flexible packaging Methods 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 208000016361 genetic disease Diseases 0.000 description 1
- 230000007614 genetic variation Effects 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 229960002048 guanfacine Drugs 0.000 description 1
- FMPNFDSPHNUFOS-LPJDIUFZSA-N himbacine Chemical compound C(/[C@@H]1[C@H]2CCCC[C@@H]2C[C@@H]2C(=O)O[C@H]([C@H]12)C)=C\[C@H]1CCC[C@H](C)N1C FMPNFDSPHNUFOS-LPJDIUFZSA-N 0.000 description 1
- 201000006318 hyperopia Diseases 0.000 description 1
- 230000004305 hyperopia Effects 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 230000000366 juvenile effect Effects 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- GGXICVAJURFBLW-CEYXHVGTSA-N latanoprost Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCC1=CC=CC=C1 GGXICVAJURFBLW-CEYXHVGTSA-N 0.000 description 1
- 229960001160 latanoprost Drugs 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000010197 meta-analysis Methods 0.000 description 1
- MFUKVPOVVKKLRQ-UHFFFAOYSA-N methyl(1,2,3,6-tetrahydropyridin-1-ium-4-yl)phosphinate Chemical compound CP(O)(=O)C1=CCNCC1 MFUKVPOVVKKLRQ-UHFFFAOYSA-N 0.000 description 1
- BCDIWLCKOCHCIH-UHFFFAOYSA-N methylphosphinic acid Chemical compound CP(O)=O BCDIWLCKOCHCIH-UHFFFAOYSA-N 0.000 description 1
- 230000002911 mydriatic effect Effects 0.000 description 1
- 102000039446 nucleic acids Human genes 0.000 description 1
- 108020004707 nucleic acids Proteins 0.000 description 1
- 150000007523 nucleic acids Chemical class 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 210000001328 optic nerve Anatomy 0.000 description 1
- 230000008520 organization Effects 0.000 description 1
- 230000035479 physiological effects, processes and functions Effects 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 230000005180 public health Effects 0.000 description 1
- 239000000296 purinergic P1 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000009877 rendering Methods 0.000 description 1
- 230000004264 retinal detachment Effects 0.000 description 1
- 201000007714 retinoschisis Diseases 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000004088 simulation Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
- 229960004559 theobromine Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000008719 thickening Effects 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 230000004382 visual function Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
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
- A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
-
- 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
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia
Landscapes
- 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)
- Ophthalmology & Optometry (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)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063037910P | 2020-06-11 | 2020-06-11 | |
| US63/037,910 | 2020-06-11 | ||
| PCT/US2021/036628 WO2021252636A1 (en) | 2020-06-11 | 2021-06-09 | Methods and compositions for preventing and treating myopia with fingolimod, a sphingosine-1-phosphate receptor modulator, and derivatives thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3182431A1 true CA3182431A1 (en) | 2021-12-16 |
Family
ID=78846511
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3182431A Pending CA3182431A1 (en) | 2020-06-11 | 2021-06-09 | Methods and compositions for preventing and treating myopia with fingolimod, a sphingosine-1-phosphate receptor modulator, and derivatives thereof |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP4164605A4 (zh) |
| JP (1) | JP2023530681A (zh) |
| KR (1) | KR20230051154A (zh) |
| CN (1) | CN116133665A (zh) |
| CA (1) | CA3182431A1 (zh) |
| IL (1) | IL298996A (zh) |
| WO (1) | WO2021252636A1 (zh) |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0504544D0 (en) * | 2005-03-04 | 2005-04-13 | Novartis Ag | Organic compounds |
| US9827250B2 (en) * | 2012-07-31 | 2017-11-28 | Johnson & Johnson Vision Care, Inc. | Lens incorporating myopia control optics and muscarinic agents |
| WO2015138700A1 (en) * | 2014-03-13 | 2015-09-17 | Bodor Laboratories, Inc. | Use of selected anticholinergic zwitterions |
| WO2016172712A2 (en) * | 2015-04-23 | 2016-10-27 | Sydnexis, Inc. | Ophthalmic composition |
| SG11202006255UA (en) * | 2018-02-02 | 2020-07-29 | Univ Kyoto | Medicine for preventing or treating ophthalmic disease associated with enhanced intraocular neovascularization and/or intraocular vascular permeability |
-
2021
- 2021-06-09 CN CN202180058323.4A patent/CN116133665A/zh active Pending
- 2021-06-09 EP EP21821401.3A patent/EP4164605A4/en active Pending
- 2021-06-09 KR KR1020237001145A patent/KR20230051154A/ko unknown
- 2021-06-09 JP JP2022576467A patent/JP2023530681A/ja active Pending
- 2021-06-09 IL IL298996A patent/IL298996A/en unknown
- 2021-06-09 CA CA3182431A patent/CA3182431A1/en active Pending
- 2021-06-09 WO PCT/US2021/036628 patent/WO2021252636A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20230051154A (ko) | 2023-04-17 |
| CN116133665A (zh) | 2023-05-16 |
| EP4164605A4 (en) | 2024-06-19 |
| EP4164605A1 (en) | 2023-04-19 |
| JP2023530681A (ja) | 2023-07-19 |
| IL298996A (en) | 2023-02-01 |
| WO2021252636A1 (en) | 2021-12-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Upadhyay et al. | Biological mechanisms of atropine control of myopia | |
| Wildsoet et al. | IMI–interventions for controlling myopia onset and progression report | |
| Mak et al. | Epidemiology of myopia and prevention of myopia progression in children in East Asia: a review | |
| Pugazhendhi et al. | Pathogenesis and prevention of worsening axial elongation in pathological myopia | |
| Russo et al. | Myopia onset and progression: can it be prevented? | |
| Tkatchenko et al. | Pharmacogenomic approach to antimyopia drug development: pathways lead the way | |
| US20230138414A1 (en) | Methods and compositions for preventing and treating myopia | |
| CA3182431A1 (en) | Methods and compositions for preventing and treating myopia with fingolimod, a sphingosine-1-phosphate receptor modulator, and derivatives thereof | |
| CA3182439A1 (en) | Methods and compositions for preventing and treating myopia with s-methyl-l-thiocitrulline, a selective neuronal nitric oxide synthase (nnos) inhibitor, and derivatives thereof | |
| CA3182437A1 (en) | Methods and compositions for preventing and treating myopia with berberine, a berberidaceaen alkaloid, and derivatives thereof | |
| CA3181292A1 (en) | Methods and compositions for preventing and treating myopia with levocabastine, a selective histamine h1-receptor antagonist, and derivatives thereof | |
| CA3182426A1 (en) | Methods and compositions for preventing and treating myopia with trichostatin a, a histone deacetylase (hdac) inhibitor, and derivatives thereof | |
| CA3182397A1 (en) | Methods and compositions for preventing and treating myopia with fenoterol hydrobromide, a .beta.2-adrenergic receptor agonist, and derivatives thereof | |
| Garcia et al. | Prevention of myopia progression using orthokeratology | |
| Kresch | The myopia epidemic: Are new therapies in sight? |