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dapsone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antimycobacterials, diaminodiphenylsulfone derivatives | 782 | 80-08-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A sulfone active against a wide range of bacteria but mainly employed for its actions against MYCOBACTERIUM LEPRAE. Its mechanism of action is probably similar to that of the SULFONAMIDES which involves inhibition of folic acid synthesis in susceptible organisms. It is also used with PYRIMETHAMINE in the treatment of malaria. (From Martindale, The Extra Pharmacopoeia, 30th ed, p157-8)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.20 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 15 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 20.14 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 93 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.83 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.48 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.25 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 22 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.775 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.929 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 49.888 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.582 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 53.050 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 81.980 | % | High | 1 |
| herg | hERG pIC50 | 4.020 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.704 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.020 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 51.090 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAPK1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 58 | |||
| kinase-selectivity-class | AURKA,DDR1,DYRK1B,ERBB2,GRK2,MAP2K3,MAP2K6,MAPK7,PDK2,PDK4,SIK2,STK33,TEK,TTK | 14 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 1.449 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 6.383 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 9.247 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 46.440 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 7.762 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 53.560 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.215 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 12.388 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 91.850 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 38.850 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 183.654 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 3, 1979 | FDA | JACOBUS |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Methaemoglobinaemia | 1390.74 | 15.46 | 270 | 12884 | 3745 | 90611548 |
| Drug reaction with eosinophilia and systemic symptoms | 380.15 | 15.46 | 164 | 12990 | 42594 | 90572699 |
| Off label use | 282.51 | 15.46 | 540 | 12614 | 1101712 | 89513581 |
| Haemolytic anaemia | 192.22 | 15.46 | 70 | 13084 | 11627 | 90603666 |
| Drug ineffective for unapproved indication | 138.90 | 15.46 | 98 | 13056 | 66546 | 90548747 |
| Drug ineffective | 136.65 | 15.46 | 474 | 12680 | 1383824 | 89231469 |
| Treatment failure | 130.91 | 15.46 | 189 | 12965 | 303739 | 90311554 |
| Linear IgA disease | 128.61 | 15.46 | 35 | 13119 | 2239 | 90613054 |
| Haemolysis | 76.69 | 15.46 | 33 | 13121 | 8477 | 90606816 |
| Blood methaemoglobin present | 75.26 | 15.46 | 13 | 13141 | 88 | 90615205 |
| Rebound effect | 64.16 | 15.46 | 30 | 13124 | 9354 | 90605939 |
| Product use in unapproved indication | 62.06 | 15.46 | 145 | 13009 | 336091 | 90279202 |
| Sepsis | 59.29 | 15.46 | 99 | 13055 | 179715 | 90435578 |
| Chronic spontaneous urticaria | 58.27 | 15.46 | 18 | 13136 | 1802 | 90613491 |
| Eyelid irritation | 54.61 | 15.46 | 15 | 13139 | 993 | 90614300 |
| Type 2 lepra reaction | 52.49 | 15.46 | 9 | 13145 | 58 | 90615235 |
| Cytomegalovirus infection | 48.27 | 15.46 | 36 | 13118 | 26566 | 90588727 |
| Angioedema | 48.07 | 15.46 | 53 | 13101 | 64823 | 90550470 |
| Hydronephrosis | 47.94 | 15.46 | 27 | 13127 | 12375 | 90602918 |
| Skin odour abnormal | 45.74 | 15.46 | 15 | 13139 | 1820 | 90613473 |
| Hypoxia | 44.97 | 15.46 | 54 | 13100 | 72345 | 90542948 |
| Therapy partial responder | 44.92 | 15.46 | 32 | 13122 | 22011 | 90593282 |
| Myopathy | 43.17 | 15.46 | 26 | 13128 | 13492 | 90601801 |
| Serotonin syndrome | 40.99 | 15.46 | 38 | 13116 | 37849 | 90577444 |
| Mental disorder | 38.07 | 15.46 | 34 | 13120 | 32284 | 90583009 |
| Arthropathy | 36.43 | 15.46 | 5 | 13149 | 366237 | 90249056 |
| Joint swelling | 36.05 | 15.46 | 14 | 13140 | 503286 | 90112007 |
| Cushingoid | 35.82 | 15.46 | 21 | 13133 | 10374 | 90604919 |
| Contraindicated product administered | 35.32 | 15.46 | 3 | 13151 | 320136 | 90295157 |
| Lymphadenitis | 33.88 | 15.46 | 15 | 13139 | 4122 | 90611171 |
| Oxygen saturation decreased | 32.52 | 15.46 | 57 | 13097 | 107426 | 90507867 |
| Wound complication | 31.86 | 15.46 | 15 | 13139 | 4748 | 90610545 |
| Disease recurrence | 31.83 | 15.46 | 33 | 13121 | 37620 | 90577673 |
| Hepatitis fulminant | 31.33 | 15.46 | 14 | 13140 | 3931 | 90611362 |
| Wound secretion | 31.19 | 15.46 | 15 | 13139 | 4975 | 90610318 |
| Therapeutic product ineffective | 30.76 | 15.46 | 12 | 13142 | 2402 | 90612891 |
| Idiopathic pneumonia syndrome | 30.51 | 15.46 | 8 | 13146 | 443 | 90614850 |
| Thyroid tuberculosis | 30.24 | 15.46 | 5 | 13149 | 25 | 90615268 |
| Anaemia | 30.22 | 15.46 | 116 | 13038 | 352686 | 90262607 |
| Abdominal discomfort | 29.94 | 15.46 | 16 | 13138 | 477312 | 90137981 |
| Type IIb hyperlipidaemia | 29.47 | 15.46 | 5 | 13149 | 30 | 90615263 |
| Therapy non-responder | 28.55 | 15.46 | 62 | 13092 | 136642 | 90478651 |
| Product prescribing issue | 24.59 | 15.46 | 15 | 13139 | 7964 | 90607329 |
| Pseudomonas infection | 24.50 | 15.46 | 19 | 13135 | 14846 | 90600447 |
| Cyanosis | 23.97 | 15.46 | 21 | 13133 | 19434 | 90595859 |
| Dermatitis | 23.48 | 15.46 | 22 | 13132 | 22198 | 90593095 |
| Psoriatic arthropathy | 22.97 | 15.46 | 3 | 13151 | 228332 | 90386961 |
| Type 1 diabetes mellitus | 22.83 | 15.46 | 12 | 13142 | 4800 | 90610493 |
| Leukopenia | 22.55 | 15.46 | 47 | 13107 | 100663 | 90514630 |
| Skin lesion | 21.78 | 15.46 | 27 | 13127 | 37338 | 90577955 |
| Subcutaneous abscess | 21.75 | 15.46 | 13 | 13141 | 6653 | 90608640 |
| Rheumatoid arthritis | 21.51 | 15.46 | 13 | 13141 | 362601 | 90252692 |
| Skin hyperpigmentation | 21.42 | 15.46 | 13 | 13141 | 6838 | 90608455 |
| Klebsiella infection | 21.10 | 15.46 | 15 | 13139 | 10282 | 90605011 |
| Discomfort | 20.69 | 15.46 | 7 | 13147 | 274328 | 90340965 |
| Accidental poisoning | 20.56 | 15.46 | 7 | 13147 | 953 | 90614340 |
| Drug interaction | 20.54 | 15.46 | 87 | 13067 | 276366 | 90338927 |
| Congenital hydrocephalus | 20.37 | 15.46 | 5 | 13149 | 212 | 90615081 |
| Pancytopenia | 20.12 | 15.46 | 50 | 13104 | 120213 | 90495080 |
| Arthralgia | 20.01 | 15.46 | 53 | 13101 | 778469 | 89836824 |
| Rash maculo-papular | 19.83 | 15.46 | 27 | 13127 | 40906 | 90574387 |
| Scar | 19.74 | 15.46 | 17 | 13137 | 15378 | 90599915 |
| Drug effective for unapproved indication | 19.69 | 15.46 | 13 | 13141 | 7905 | 90607388 |
| Infusion related reaction | 19.56 | 15.46 | 19 | 13135 | 416761 | 90198532 |
| Wound | 19.21 | 15.46 | 10 | 13144 | 302970 | 90312323 |
| Stomatitis | 19.06 | 15.46 | 8 | 13146 | 274690 | 90340603 |
| Eosinophilic myocarditis | 18.70 | 15.46 | 6 | 13148 | 679 | 90614614 |
| Osteonecrosis | 18.67 | 15.46 | 21 | 13133 | 26220 | 90589073 |
| Musculoskeletal stiffness | 18.49 | 15.46 | 10 | 13144 | 296522 | 90318771 |
| Cutaneous lupus erythematosus | 18.37 | 15.46 | 9 | 13145 | 3109 | 90612184 |
| Marrow hyperplasia | 18.10 | 15.46 | 6 | 13148 | 753 | 90614540 |
| Pyoderma gangrenosum | 18.02 | 15.46 | 10 | 13144 | 4454 | 90610839 |
| Skin exfoliation | 17.98 | 15.46 | 34 | 13120 | 67879 | 90547414 |
| Blood creatinine increased | 17.86 | 15.46 | 43 | 13111 | 101343 | 90513950 |
| Calciphylaxis | 17.69 | 15.46 | 9 | 13145 | 3367 | 90611926 |
| Pemphigus | 17.66 | 15.46 | 13 | 13141 | 326851 | 90288442 |
| Bronchopulmonary aspergillosis | 17.56 | 15.46 | 14 | 13140 | 11384 | 90603909 |
| Hepatic enzyme increased | 17.44 | 15.46 | 16 | 13138 | 360720 | 90254573 |
| CD4 lymphocytes decreased | 17.30 | 15.46 | 7 | 13147 | 1540 | 90613753 |
| Application site exfoliation | 16.90 | 15.46 | 5 | 13149 | 432 | 90614861 |
| Sinusitis | 16.84 | 15.46 | 15 | 13139 | 343073 | 90272220 |
| Choriomeningitis lymphocytic | 16.82 | 15.46 | 3 | 13151 | 25 | 90615268 |
| Granulomatous liver disease | 16.78 | 15.46 | 6 | 13148 | 943 | 90614350 |
| Methylobacterium infection | 16.61 | 15.46 | 3 | 13151 | 27 | 90615266 |
| Necrotising fasciitis | 16.51 | 15.46 | 9 | 13145 | 3871 | 90611422 |
| Therapeutic product effect decreased | 16.39 | 15.46 | 10 | 13144 | 277561 | 90337732 |
| Disease progression | 16.37 | 15.46 | 55 | 13099 | 156560 | 90458733 |
| Superinfection bacterial | 16.35 | 15.46 | 6 | 13148 | 1016 | 90614277 |
| Blood cholesterol increased | 16.23 | 15.46 | 5 | 13149 | 208007 | 90407286 |
| Maternal exposure during pregnancy | 16.22 | 15.46 | 17 | 13137 | 360046 | 90255247 |
| Product delivery mechanism issue | 16.08 | 15.46 | 5 | 13149 | 511 | 90614782 |
| Emotional distress | 16 | 15.46 | 23 | 13131 | 36639 | 90578654 |
| Pemphigoid | 15.89 | 15.46 | 12 | 13142 | 9014 | 90606279 |
| Autoimmune haemolytic anaemia | 15.84 | 15.46 | 10 | 13144 | 5635 | 90609658 |
| Dermatitis herpetiformis | 15.68 | 15.46 | 3 | 13151 | 38 | 90615255 |
| Type 2 diabetes mellitus | 15.65 | 15.46 | 5 | 13149 | 203239 | 90412054 |
| Hidradenitis | 15.55 | 15.46 | 9 | 13145 | 4338 | 90610955 |
| Condition aggravated | 15.55 | 15.46 | 143 | 13011 | 595402 | 90019891 |
| Swelling | 15.51 | 15.46 | 23 | 13131 | 419035 | 90196258 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Methaemoglobinaemia | 535.43 | 15.98 | 149 | 11167 | 5625 | 42604394 |
| Drug reaction with eosinophilia and systemic symptoms | 233.53 | 15.98 | 143 | 11173 | 41932 | 42568087 |
| Haemolytic anaemia | 148.96 | 15.98 | 70 | 11246 | 12057 | 42597962 |
| Type 2 lepra reaction | 137.27 | 15.98 | 29 | 11287 | 326 | 42609693 |
| Drug ineffective for unapproved indication | 73.29 | 15.98 | 75 | 11241 | 46088 | 42563931 |
| Type 1 lepra reaction | 67.52 | 15.98 | 12 | 11304 | 48 | 42609971 |
| Vanishing bile duct syndrome | 65.73 | 15.98 | 23 | 11293 | 1848 | 42608171 |
| Haemolysis | 56.71 | 15.98 | 34 | 11282 | 9555 | 42600464 |
| Nocardiosis | 54.74 | 15.98 | 27 | 11289 | 5163 | 42604856 |
| Drug ineffective | 54.55 | 15.98 | 318 | 10998 | 629879 | 41980140 |
| Rebound effect | 51.14 | 15.98 | 29 | 11287 | 7350 | 42602669 |
| Mycobacterium avium complex infection | 48.35 | 15.98 | 21 | 11295 | 3006 | 42607013 |
| Off label use | 48.18 | 15.98 | 311 | 11005 | 638024 | 41971995 |
| Treatment failure | 47.38 | 15.98 | 70 | 11246 | 62554 | 42547465 |
| Pleocytosis | 43.07 | 15.98 | 13 | 11303 | 652 | 42609367 |
| Brain abscess | 41.39 | 15.98 | 21 | 11295 | 4263 | 42605756 |
| Anaemia Heinz body | 40.70 | 15.98 | 7 | 11309 | 22 | 42609997 |
| Pyrexia | 37.97 | 15.98 | 205 | 11111 | 393837 | 42216182 |
| Blood methaemoglobin present | 37.32 | 15.98 | 7 | 11309 | 40 | 42609979 |
| Glucose tolerance impaired | 33.50 | 15.98 | 18 | 11298 | 4106 | 42605913 |
| Drug-induced liver injury | 32.18 | 15.98 | 45 | 11271 | 38228 | 42571791 |
| HIV associated nephropathy | 32.15 | 15.98 | 9 | 11307 | 345 | 42609674 |
| Aeromonas infection | 32.00 | 15.98 | 9 | 11307 | 351 | 42609668 |
| Hypoxia | 29.11 | 15.98 | 60 | 11256 | 69726 | 42540293 |
| Leukaemoid reaction | 28.95 | 15.98 | 7 | 11309 | 149 | 42609870 |
| Cataract | 27.25 | 15.98 | 37 | 11279 | 30567 | 42579452 |
| Necrotising fasciitis | 26.57 | 15.98 | 16 | 11300 | 4530 | 42605489 |
| Pancytopenia | 25.60 | 15.98 | 79 | 11237 | 117664 | 42492355 |
| Toxoplasmosis | 25.18 | 15.98 | 11 | 11305 | 1596 | 42608423 |
| Bone marrow failure | 25.02 | 15.98 | 37 | 11279 | 33056 | 42576963 |
| Papillary cystadenoma lymphomatosum | 24.38 | 15.98 | 5 | 11311 | 48 | 42609971 |
| Meningitis aseptic | 24.21 | 15.98 | 15 | 11301 | 4467 | 42605552 |
| Epstein-Barr virus infection | 23.55 | 15.98 | 20 | 11296 | 9698 | 42600321 |
| Fluid imbalance | 23.02 | 15.98 | 7 | 11309 | 360 | 42609659 |
| Pneumonia pseudomonal | 22.96 | 15.98 | 15 | 11301 | 4894 | 42605125 |
| Death | 22.72 | 15.98 | 58 | 11258 | 471127 | 42138892 |
| Cushingoid | 22.51 | 15.98 | 13 | 11303 | 3409 | 42606610 |
| Thrombocytopenia | 22.47 | 15.98 | 105 | 11211 | 190174 | 42419845 |
| Photophobia | 22.37 | 15.98 | 18 | 11298 | 8101 | 42601918 |
| Induration | 22.07 | 15.98 | 9 | 11307 | 1101 | 42608918 |
| Autoinflammatory disease | 21.80 | 15.98 | 5 | 11311 | 84 | 42609935 |
| Jarisch-Herxheimer reaction | 21.22 | 15.98 | 8 | 11308 | 795 | 42609224 |
| Pneumocystis jirovecii pneumonia | 20.26 | 15.98 | 29 | 11287 | 25152 | 42584867 |
| Therapy non-responder | 20.07 | 15.98 | 44 | 11272 | 53315 | 42556704 |
| Mucormycosis | 20.03 | 15.98 | 16 | 11300 | 7127 | 42602892 |
| Vascular cognitive impairment | 19.36 | 15.98 | 4 | 11312 | 40 | 42609979 |
| Scrotal cyst | 18.98 | 15.98 | 5 | 11311 | 152 | 42609867 |
| Mycobacterium abscessus infection | 18.03 | 15.98 | 7 | 11309 | 753 | 42609266 |
| Chronic myelomonocytic leukaemia | 18.00 | 15.98 | 7 | 11309 | 756 | 42609263 |
| Tuberculoid leprosy | 17.45 | 15.98 | 4 | 11312 | 67 | 42609952 |
| Disseminated cryptococcosis | 17.33 | 15.98 | 9 | 11307 | 1916 | 42608103 |
| Injection site reaction | 17.12 | 15.98 | 21 | 11295 | 15700 | 42594319 |
| Blister | 16.96 | 15.98 | 28 | 11288 | 27462 | 42582557 |
| Malignant neoplasm progression | 16.91 | 15.98 | 4 | 11312 | 108396 | 42501623 |
| Pneumonia cryptococcal | 16.36 | 15.98 | 8 | 11308 | 1500 | 42608519 |
| Dermatitis exfoliative | 16.23 | 15.98 | 14 | 11302 | 6933 | 42603086 |
| Choroidal effusion | 16.15 | 15.98 | 5 | 11311 | 273 | 42609746 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Methaemoglobinaemia | 1702.38 | 14.30 | 385 | 20422 | 8783 | 110559709 |
| Drug reaction with eosinophilia and systemic symptoms | 628.28 | 14.30 | 307 | 20500 | 81788 | 110486704 |
| Haemolytic anaemia | 315.03 | 14.30 | 126 | 20681 | 20794 | 110547698 |
| Off label use | 263.61 | 14.30 | 743 | 20064 | 1499442 | 109069050 |
| Drug ineffective for unapproved indication | 193.61 | 14.30 | 158 | 20649 | 102680 | 110465812 |
| Type 2 lepra reaction | 178.80 | 14.30 | 35 | 20772 | 380 | 110568112 |
| Drug ineffective | 153.11 | 14.30 | 626 | 20181 | 1519914 | 109048578 |
| Treatment failure | 145.17 | 14.30 | 217 | 20590 | 277017 | 110291475 |
| Haemolysis | 126.95 | 14.30 | 61 | 20746 | 15578 | 110552914 |
| Rebound effect | 111.91 | 14.30 | 55 | 20752 | 14751 | 110553741 |
| Linear IgA disease | 108.36 | 14.30 | 38 | 20769 | 4351 | 110564141 |
| Blood methaemoglobin present | 103.54 | 14.30 | 19 | 20788 | 141 | 110568351 |
| Type 1 lepra reaction | 88.03 | 14.30 | 15 | 20792 | 68 | 110568424 |
| Nocardiosis | 69.37 | 14.30 | 32 | 20775 | 7454 | 110561038 |
| Hypoxia | 65.70 | 14.30 | 100 | 20707 | 129415 | 110439077 |
| Vanishing bile duct syndrome | 65.30 | 14.30 | 24 | 20783 | 3144 | 110565348 |
| Cushingoid | 58.54 | 14.30 | 33 | 20774 | 11679 | 110556813 |
| Sepsis | 58.46 | 14.30 | 164 | 20643 | 327182 | 110241310 |
| Product use in unapproved indication | 55.86 | 14.30 | 198 | 20609 | 447179 | 110121313 |
| Therapy partial responder | 51.61 | 14.30 | 48 | 20759 | 37013 | 110531479 |
| Eyelid irritation | 49.05 | 14.30 | 15 | 20792 | 1116 | 110567376 |
| Therapy non-responder | 49.05 | 14.30 | 98 | 20709 | 157209 | 110411283 |
| Anaemia | 47.34 | 14.30 | 216 | 20591 | 546870 | 110021622 |
| Pancytopenia | 46.58 | 14.30 | 114 | 20693 | 209499 | 110358993 |
| Disease recurrence | 46.04 | 14.30 | 57 | 20750 | 60727 | 110507765 |
| Chronic spontaneous urticaria | 44.44 | 14.30 | 16 | 20791 | 1977 | 110566515 |
| Joint swelling | 42.71 | 14.30 | 15 | 20792 | 442830 | 110125662 |
| Leukaemoid reaction | 42.53 | 14.30 | 11 | 20796 | 443 | 110568049 |
| Pyrexia | 42.16 | 14.30 | 301 | 20506 | 897964 | 109670528 |
| Anaemia Heinz body | 41.79 | 14.30 | 7 | 20800 | 28 | 110568464 |
| Cytomegalovirus infection | 41.15 | 14.30 | 51 | 20756 | 54393 | 110514099 |
| Brain abscess | 39.13 | 14.30 | 21 | 20786 | 6753 | 110561739 |
| Mycobacterium avium complex infection | 39.02 | 14.30 | 20 | 20787 | 5857 | 110562635 |
| Drug-induced liver injury | 38.86 | 14.30 | 76 | 20731 | 119991 | 110448501 |
| Necrotising fasciitis | 36.89 | 14.30 | 21 | 20786 | 7570 | 110560922 |
| Pseudomonas infection | 36.73 | 14.30 | 35 | 20772 | 27818 | 110540674 |
| Myopathy | 36.06 | 14.30 | 33 | 20774 | 24927 | 110543565 |
| Drug effective for unapproved indication | 35.90 | 14.30 | 26 | 20781 | 14141 | 110554351 |
| Contraindicated product administered | 35.52 | 14.30 | 3 | 20804 | 248264 | 110320228 |
| Pleocytosis | 35.31 | 14.30 | 13 | 20794 | 1711 | 110566781 |
| HIV associated nephropathy | 35.03 | 14.30 | 9 | 20798 | 353 | 110568139 |
| Therapeutic product ineffective | 33.43 | 14.30 | 14 | 20793 | 2590 | 110565902 |
| Hydronephrosis | 33.18 | 14.30 | 29 | 20778 | 20636 | 110547856 |
| Pneumocystis jirovecii pneumonia | 32.24 | 14.30 | 40 | 20767 | 42695 | 110525797 |
| Aeromonas infection | 31.51 | 14.30 | 9 | 20798 | 528 | 110567964 |
| Cyanosis | 31.17 | 14.30 | 33 | 20774 | 29708 | 110538784 |
| Skin odour abnormal | 30.86 | 14.30 | 13 | 20794 | 2441 | 110566051 |
| Pneumonia pseudomonal | 29.14 | 14.30 | 18 | 20789 | 7528 | 110560964 |
| Thyroid tuberculosis | 28.62 | 14.30 | 5 | 20802 | 27 | 110568465 |
| Type IIb hyperlipidaemia | 28.03 | 14.30 | 5 | 20802 | 31 | 110568461 |
| Infusion related reaction | 27.55 | 14.30 | 19 | 20788 | 381143 | 110187349 |
| Epstein-Barr virus infection | 27.51 | 14.30 | 25 | 20782 | 18713 | 110549779 |
| Rheumatoid arthritis | 27.45 | 14.30 | 11 | 20796 | 299602 | 110268890 |
| Arthralgia | 26.56 | 14.30 | 68 | 20739 | 779564 | 109788928 |
| Psoriatic arthropathy | 26.51 | 14.30 | 3 | 20804 | 196758 | 110371734 |
| Cutaneous lupus erythematosus | 26.48 | 14.30 | 13 | 20794 | 3475 | 110565017 |
| Staphylococcal infection | 26.02 | 14.30 | 47 | 20760 | 69897 | 110498595 |
| Leukocytosis | 25.09 | 14.30 | 40 | 20767 | 53788 | 110514704 |
| Jaundice | 24.89 | 14.30 | 42 | 20765 | 59194 | 110509298 |
| Product prescribing issue | 24.79 | 14.30 | 20 | 20787 | 12752 | 110555740 |
| Osteonecrosis | 24.52 | 14.30 | 31 | 20776 | 33710 | 110534782 |
| Peripheral swelling | 24.41 | 14.30 | 24 | 20783 | 404010 | 110164482 |
| Jarisch-Herxheimer reaction | 24.27 | 14.30 | 9 | 20798 | 1208 | 110567284 |
| Dermatitis | 24.19 | 14.30 | 28 | 20779 | 27809 | 110540683 |
| Arthropathy | 24.07 | 14.30 | 12 | 20795 | 287510 | 110280982 |
| Therapeutic product effect decreased | 24.01 | 14.30 | 8 | 20799 | 244308 | 110324184 |
| Thrombocytopenia | 23.89 | 14.30 | 129 | 20678 | 348756 | 110219736 |
| Completed suicide | 23.71 | 14.30 | 8 | 20799 | 242373 | 110326119 |
| Leukopenia | 23.12 | 14.30 | 71 | 20736 | 148720 | 110419772 |
| Pain in extremity | 23.04 | 14.30 | 35 | 20772 | 487083 | 110081409 |
| Discomfort | 22.98 | 14.30 | 6 | 20801 | 214701 | 110353791 |
| Mucocutaneous leishmaniasis | 22.85 | 14.30 | 7 | 20800 | 524 | 110567968 |
| Rash maculo-papular | 22.83 | 14.30 | 46 | 20761 | 74176 | 110494316 |
| Tuberculoid leprosy | 22.15 | 14.30 | 5 | 20802 | 112 | 110568380 |
| Abdominal discomfort | 22.00 | 14.30 | 25 | 20782 | 393833 | 110174659 |
| Pain | 21.82 | 14.30 | 99 | 20708 | 954856 | 109613636 |
| Lung infiltration | 21.78 | 14.30 | 25 | 20782 | 24603 | 110543889 |
| Osteoarthritis | 21.78 | 14.30 | 4 | 20803 | 182619 | 110385873 |
| Helicobacter infection | 21.66 | 14.30 | 4 | 20803 | 181873 | 110386619 |
| Stomatitis | 21.56 | 14.30 | 12 | 20795 | 270230 | 110298262 |
| Induration | 21.47 | 14.30 | 10 | 20797 | 2379 | 110566113 |
| Mucormycosis | 21.39 | 14.30 | 17 | 20790 | 10611 | 110557881 |
| Serotonin syndrome | 21.05 | 14.30 | 39 | 20768 | 59114 | 110509378 |
| Fluid imbalance | 20.93 | 14.30 | 7 | 20800 | 695 | 110567797 |
| Skin lesion | 20.89 | 14.30 | 36 | 20771 | 51595 | 110516897 |
| Skin exfoliation | 20.88 | 14.30 | 49 | 20758 | 87602 | 110480890 |
| Respiratory failure | 20.83 | 14.30 | 88 | 20719 | 215244 | 110353248 |
| Wound secretion | 20.59 | 14.30 | 14 | 20793 | 6887 | 110561605 |
| Meningitis aseptic | 20.32 | 14.30 | 16 | 20791 | 9854 | 110558638 |
| Asthma | 20.13 | 14.30 | 11 | 20796 | 250280 | 110318212 |
| Vascular cognitive impairment | 20.06 | 14.30 | 4 | 20803 | 48 | 110568444 |
| Musculoskeletal pain | 19.81 | 14.30 | 5 | 20802 | 183018 | 110385474 |
| Wheezing | 19.41 | 14.30 | 12 | 20795 | 255218 | 110313274 |
| Type 1 diabetes mellitus | 19.35 | 14.30 | 15 | 20792 | 9032 | 110559460 |
| Idiopathic pneumonia syndrome | 19.32 | 14.30 | 7 | 20800 | 880 | 110567612 |
| Renal failure | 19.19 | 14.30 | 89 | 20718 | 226485 | 110342007 |
| Papillary cystadenoma lymphomatosum | 19.06 | 14.30 | 5 | 20802 | 213 | 110568279 |
| Nasopharyngitis | 18.96 | 14.30 | 28 | 20779 | 394333 | 110174159 |
| Sleep disorder | 18.67 | 14.30 | 7 | 20800 | 198637 | 110369855 |
| Toxoplasmosis | 18.59 | 14.30 | 10 | 20797 | 3229 | 110565263 |
| Pyoderma gangrenosum | 18.49 | 14.30 | 12 | 20795 | 5464 | 110563028 |
| Graft versus host disease | 18.19 | 14.30 | 20 | 20787 | 18786 | 110549706 |
| Plasma cell myeloma | 18.17 | 14.30 | 38 | 20769 | 62898 | 110505594 |
| Accidental poisoning | 18.08 | 14.30 | 9 | 20798 | 2478 | 110566014 |
| Hepatitis fulminant | 17.89 | 14.30 | 14 | 20793 | 8546 | 110559946 |
| Lupus nephritis | 17.74 | 14.30 | 11 | 20796 | 4634 | 110563858 |
| Musculoskeletal stiffness | 17.62 | 14.30 | 16 | 20791 | 279806 | 110288686 |
| Polychromasia | 17.56 | 14.30 | 6 | 20801 | 635 | 110567857 |
| Disseminated cryptococcosis | 17.52 | 14.30 | 9 | 20798 | 2648 | 110565844 |
| Pemphigoid | 17.42 | 14.30 | 20 | 20787 | 19687 | 110548805 |
| Klebsiella infection | 17.17 | 14.30 | 20 | 20787 | 19989 | 110548503 |
| Acute respiratory failure | 16.77 | 14.30 | 41 | 20766 | 75219 | 110493273 |
| Maternal exposure during pregnancy | 16.75 | 14.30 | 14 | 20793 | 254869 | 110313623 |
| Lymphocytic infiltration | 16.74 | 14.30 | 8 | 20799 | 2017 | 110566475 |
| Lepromatous leprosy | 16.63 | 14.30 | 4 | 20803 | 119 | 110568373 |
| Staphylococcal bacteraemia | 16.58 | 14.30 | 18 | 20789 | 16670 | 110551822 |
| CD4 lymphocytes decreased | 16.56 | 14.30 | 9 | 20798 | 2965 | 110565527 |
| Calciphylaxis | 16.20 | 14.30 | 10 | 20797 | 4177 | 110564315 |
| Swelling | 15.85 | 14.30 | 26 | 20781 | 351015 | 110217477 |
| Methylobacterium infection | 15.83 | 14.30 | 3 | 20804 | 27 | 110568465 |
| Cytomegalovirus test positive | 15.78 | 14.30 | 12 | 20795 | 7024 | 110561468 |
| Clostridium difficile colitis | 15.75 | 14.30 | 29 | 20778 | 43749 | 110524743 |
| Clostridium difficile infection | 15.66 | 14.30 | 32 | 20775 | 52097 | 110516395 |
| Skin hyperpigmentation | 15.58 | 14.30 | 13 | 20794 | 8683 | 110559809 |
| Osteopenia | 15.50 | 14.30 | 20 | 20787 | 22189 | 110546303 |
| Eosinophilic pustular folliculitis | 15.47 | 14.30 | 4 | 20803 | 161 | 110568331 |
| Granulomatous liver disease | 15.40 | 14.30 | 7 | 20800 | 1577 | 110566915 |
| Autoimmune haemolytic anaemia | 15.32 | 14.30 | 14 | 20793 | 10553 | 110557939 |
| Wound | 15.25 | 14.30 | 13 | 20794 | 234424 | 110334068 |
| Drug interaction | 15.06 | 14.30 | 152 | 20655 | 500031 | 110068461 |
| Oxygen saturation decreased | 15.06 | 14.30 | 64 | 20743 | 156918 | 110411574 |
| Pneumonia cryptococcal | 15.02 | 14.30 | 8 | 20799 | 2534 | 110565958 |
| Mycobacterium abscessus infection | 14.90 | 14.30 | 7 | 20800 | 1699 | 110566793 |
| Application site discolouration | 14.69 | 14.30 | 6 | 20801 | 1043 | 110567449 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | D10AX05 | DERMATOLOGICALS ANTI-ACNE PREPARATIONS ANTI-ACNE PREPARATIONS FOR TOPICAL USE Other anti-acne preparations for topical use |
| ATC | J04BA02 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF LEPRA Drugs for treatment of lepra |
| ATC | J04BA50 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF LEPRA Drugs for treatment of lepra |
| ATC | J04BA51 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF LEPRA Drugs for treatment of lepra |
| FDA CS | M0020791 | Sulfones |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000962 | Antimalarials |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D000981 | Antiprotozoal Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D005493 | Folic Acid Antagonists |
| MeSH PA | D007917 | Leprostatic Agents |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35441 | antiinfective agent |
| CHEBI has role | CHEBI:35472 | anti-inflammatory drug |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:35718 | antifungal agent |
| CHEBI has role | CHEBI:35816 | leprostatic drug |
| CHEBI has role | CHEBI:38068 | antimalarial |
| CHEBI has role | CHEBI:50177 | dermatologic drug |
| CHEBI has role | CHEBI:64946 | anti-HIV agent |
| CHEBI has role | CHEBI:233423 | antifibrotic agent |
| FDA EPC | N0000175881 | Sulfone |
Related Drugs by ATC class:
D10AX Other anti-acne preparations for topical use 5 drugs
J04BA Drugs for treatment of lepra 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Leprosy | indication | 81004002 | DOID:1024 |
| Acne vulgaris | indication | 88616000 | |
| Dermatitis herpetiformis | indication | 111196000 | DOID:8505 |
| Subcorneal pustular dermatosis | off-label use | 25147002 | DOID:8508 |
| Benign mucous membrane pemphigoid | off-label use | 34250006 | DOID:11656 |
| Systemic lupus erythematosus | off-label use | 55464009 | DOID:9074 |
| Granuloma annulare | off-label use | 65508009 | DOID:3777 |
| Pyoderma gangrenosum | off-label use | 74578003 | DOID:8553 |
| Pemphigoid | off-label use | 86142006 | |
| Actinomycotic mycetoma | off-label use | 187089001 | |
| Toxoplasmosis | off-label use | 187192000 | DOID:9965 |
| Pneumocystosis jiroveci pneumonia | off-label use | 415125002 | DOID:11339 |
| Pneumocystis Carinii Pneumonia Prevention | off-label use | ||
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Deficiency of glucose-6-phosphate dehydrogenase | contraindication | 124134002 | DOID:2862 |
| Deficiency of cytochrome-b>5< reductase | contraindication | 124184009 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Anemia | contraindication | 271737000 | DOID:2355 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.34 | Basic |
| pKa2 | 1.73 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 6.74 | CHEMBL | |||||
| Myeloperoxidase | Enzyme | IC50 | 6.38 | CHEMBL | |||||
| Glucose-6-phosphate 1-dehydrogenase | Enzyme | WOMBAT-PK | |||||||
| Cytochrome P450 3A4 | Enzyme | Ki | 4.57 | WOMBAT-PK | |||||
| Dihydropteroate synthase 1 | Enzyme | INHIBITOR | IC50 | 5.90 | WOMBAT-PK | CHEMBL | |||
| Dihydrofolate reductase | Enzyme | IC50 | 5.82 | CHEMBL | |||||
| Dihydropteroate synthetase, putative | Enzyme | IC50 | 4.91 | CHEMBL | |||||
| 6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase | Enzyme | IC50 | 4.91 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019264 | VUID |
| N0000147467 | NUI |
| D00592 | KEGG_DRUG |
| 3108 | RXNORM |
| C0010980 | UMLSCUI |
| CHEBI:4325 | CHEBI |
| CHEMBL1043 | ChEMBL_ID |
| DB00250 | DRUGBANK_ID |
| D003622 | MESH_DESCRIPTOR_UI |
| 2955 | PUBCHEM_CID |
| 10934 | IUPHAR_LIGAND_ID |
| 1676 | INN_ID |
| 8W5C518302 | UNII |
| 4536 | MMSL |
| 682 | MMSL |
| d00098 | MMSL |
| 003003 | NDDF |
| 17308007 | SNOMEDCT_US |
| 387096002 | SNOMEDCT_US |
| 4019264 | VANDF |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ACZONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0023-3670 | GEL | 50 mg | TOPICAL | NDA | 26 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-4830 | GEL | 75 mg | TOPICAL | ANDA | 25 sections |
| DAPSONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0713-0886 | GEL | 50 mg | TOPICAL | ANDA | 26 sections |
| DAPSONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-654 | TABLET | 25 mg | ORAL | ANDA | 19 sections |
| DAPSONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-655 | TABLET | 100 mg | ORAL | ANDA | 19 sections |
| dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13668-605 | GEL | 75 mg | TOPICAL | ANDA | 23 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13925-504 | TABLET | 25 mg | ORAL | ANDA | 19 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13925-505 | TABLET | 100 mg | ORAL | ANDA | 19 sections |
| ACZONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16110-367 | GEL | 50 mg | TOPICAL | NDA | 26 sections |
| Aczone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16110-526 | GEL | 75 mg | TOPICAL | NDA | 26 sections |
| Aczone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16110-526 | GEL | 75 mg | TOPICAL | NDA | 26 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-956 | GEL | 50 mg | TOPICAL | ANDA | 26 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-975 | GEL | 75 mg | TOPICAL | ANDA | 28 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21922-018 | GEL | 50 mg | TOPICAL | ANDA | 24 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21922-018 | GEL | 50 mg | TOPICAL | ANDA | 24 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29033-036 | TABLET | 25 mg | ORAL | ANDA | 18 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29033-037 | TABLET | 100 mg | ORAL | ANDA | 18 sections |
| Dapsone | Human Prescription Drug Label | 1 | 33342-534 | TABLET | 25 mg | ORAL | ANDA | 20 sections |
| Dapsone | Human Prescription Drug Label | 1 | 33342-535 | TABLET | 100 mg | ORAL | ANDA | 20 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-008 | TABLET | 25 mg | ORAL | ANDA | 22 sections |
| DAPSONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 46708-551 | GEL | 50 mg | TOPICAL | ANDA | 23 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 46708-663 | GEL | 75 mg | TOPICAL | ANDA | 15 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-1387 | GEL | 50 mg | TOPICAL | ANDA | 26 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-1388 | GEL | 75 mg | TOPICAL | ANDA | 28 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4197 | TABLET | 25 mg | ORAL | ANDA | 20 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4198 | TABLET | 100 mg | ORAL | ANDA | 20 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-5307 | GEL | 75 mg | TOPICAL | NDA authorized generic | 26 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51862-123 | GEL | 50 mg | TOPICAL | ANDA | 28 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52817-831 | GEL | 50 mg | TOPICAL | ANDA | 24 sections |
| Dapsone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52817-832 | GEL | 75 mg | TOPICAL | ANDA | 25 sections |