Stem definition | Drug id | CAS RN |
---|---|---|
neurokinin NK1 (substance P) receptor antagonist | 230 | 170729-80-3 |
Dose | Unit | Route |
---|---|---|
165 | mg | O |
150 | mg | P |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 3.34 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 62.50 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 0.94 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 1 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.05 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 13 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
March 27, 2003 | FDA | MERCK |
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 |
---|---|---|---|---|---|---|
Febrile neutropenia | 476.88 | 16.35 | 371 | 21712 | 97296 | 50485745 |
Nausea | 194.94 | 16.35 | 710 | 21373 | 704688 | 49878353 |
Mucosal inflammation | 192.19 | 16.35 | 151 | 21932 | 39991 | 50543050 |
Neutropenia | 177.51 | 16.35 | 267 | 21816 | 147698 | 50435343 |
Erythema | 158.50 | 16.35 | 252 | 21831 | 146162 | 50436879 |
Encephalopathy | 132.32 | 16.35 | 113 | 21970 | 33598 | 50549443 |
Drug ineffective | 120.48 | 16.35 | 109 | 21974 | 819224 | 49763817 |
Flushing | 107.19 | 16.35 | 139 | 21944 | 66876 | 50516165 |
Atelectasis | 105.70 | 16.35 | 77 | 22006 | 18193 | 50564848 |
Pyrexia | 104.40 | 16.35 | 383 | 21700 | 379820 | 50203221 |
Febrile bone marrow aplasia | 100.66 | 16.35 | 51 | 22032 | 6260 | 50576781 |
Computerised tomogram thorax abnormal | 99.68 | 16.35 | 33 | 22050 | 1350 | 50581691 |
Aplasia | 82.57 | 16.35 | 38 | 22045 | 3775 | 50579266 |
Neutrophil count decreased | 79.15 | 16.35 | 99 | 21984 | 45927 | 50537114 |
Hypoxia | 75.49 | 16.35 | 102 | 21981 | 51021 | 50532020 |
Bone marrow failure | 68.82 | 16.35 | 72 | 22011 | 27552 | 50555489 |
Hyponatraemia | 68.48 | 16.35 | 138 | 21945 | 96001 | 50487040 |
Gastrointestinal disorder | 65.39 | 16.35 | 134 | 21949 | 94322 | 50488719 |
Decreased appetite | 63.21 | 16.35 | 212 | 21871 | 200711 | 50382330 |
Dyspnoea | 61.82 | 16.35 | 429 | 21654 | 547179 | 50035862 |
Fall | 61.41 | 16.35 | 35 | 22048 | 334897 | 50248144 |
Hepatocellular injury | 59.98 | 16.35 | 65 | 22018 | 25882 | 50557159 |
Injection site phlebitis | 58.01 | 16.35 | 13 | 22070 | 114 | 50582927 |
Feeling hot | 57.54 | 16.35 | 78 | 22005 | 39124 | 50543917 |
Palmar-plantar erythrodysaesthesia syndrome | 54.80 | 16.35 | 55 | 22028 | 20043 | 50562998 |
Vascular pain | 52.05 | 16.35 | 17 | 22066 | 666 | 50582375 |
Vomiting | 51.34 | 16.35 | 360 | 21723 | 460398 | 50122643 |
Respiratory syncytial virus infection | 50.27 | 16.35 | 30 | 22053 | 5072 | 50577969 |
Anaphylactic shock | 49.24 | 16.35 | 52 | 22031 | 20103 | 50562938 |
Alveolitis | 47.92 | 16.35 | 23 | 22060 | 2511 | 50580530 |
Constipation | 47.34 | 16.35 | 183 | 21900 | 185525 | 50397516 |
Neuropathy peripheral | 46.66 | 16.35 | 119 | 21964 | 96638 | 50486403 |
Sense of oppression | 46.64 | 16.35 | 17 | 22066 | 928 | 50582113 |
Oral pain | 46.50 | 16.35 | 56 | 22027 | 24977 | 50558064 |
Infusion site streaking | 46.12 | 16.35 | 14 | 22069 | 430 | 50582611 |
Injection site vasculitis | 42.31 | 16.35 | 7 | 22076 | 7 | 50583034 |
Computerised tomogram thorax | 40.03 | 16.35 | 10 | 22073 | 145 | 50582896 |
Tonsillar haemorrhage | 39.99 | 16.35 | 11 | 22072 | 236 | 50582805 |
Inappropriate antidiuretic hormone secretion | 39.62 | 16.35 | 38 | 22045 | 13105 | 50569936 |
Stomatitis | 39.24 | 16.35 | 115 | 21968 | 101229 | 50481812 |
Diarrhoea | 39.16 | 16.35 | 410 | 21673 | 588066 | 49994975 |
Depression | 35.30 | 16.35 | 14 | 22069 | 165409 | 50417632 |
Chemotherapy | 33.95 | 16.35 | 15 | 22068 | 1354 | 50581687 |
Rheumatoid arthritis | 31.91 | 16.35 | 25 | 22058 | 202525 | 50380516 |
Hypersensitivity | 31.87 | 16.35 | 181 | 21902 | 214980 | 50368061 |
Gait disturbance | 31.51 | 16.35 | 13 | 22070 | 149992 | 50433049 |
Cerebellar syndrome | 31.40 | 16.35 | 19 | 22064 | 3292 | 50579749 |
Abdominal pain | 31.31 | 16.35 | 193 | 21890 | 236035 | 50347006 |
Interstitial lung disease | 30.54 | 16.35 | 70 | 22013 | 53106 | 50529935 |
Hiccups | 30.52 | 16.35 | 15 | 22068 | 1724 | 50581317 |
Toxicity to various agents | 30.11 | 16.35 | 29 | 22054 | 212470 | 50370571 |
Chest discomfort | 29.23 | 16.35 | 98 | 21985 | 92624 | 50490417 |
Intestinal strangulation | 28.95 | 16.35 | 7 | 22076 | 88 | 50582953 |
Joint swelling | 28.77 | 16.35 | 39 | 22044 | 245247 | 50337794 |
Asthma | 28.32 | 16.35 | 3 | 22080 | 89334 | 50493707 |
Thrombocytopenia | 25.61 | 16.35 | 117 | 21966 | 127556 | 50455485 |
Leukopenia | 24.58 | 16.35 | 75 | 22008 | 67453 | 50515588 |
Colony stimulating factor therapy | 24.58 | 16.35 | 8 | 22075 | 310 | 50582731 |
Hypokalaemia | 24.27 | 16.35 | 89 | 21994 | 87903 | 50495138 |
Intercepted product administration error | 24.02 | 16.35 | 6 | 22077 | 87 | 50582954 |
Infusion related reaction | 24.01 | 16.35 | 141 | 21942 | 169416 | 50413625 |
Hypomagnesaemia | 23.80 | 16.35 | 39 | 22044 | 23117 | 50559924 |
Anorectal disorder | 23.78 | 16.35 | 12 | 22071 | 1460 | 50581581 |
Bronchitis | 23.59 | 16.35 | 8 | 22075 | 104151 | 50478890 |
Dental fistula | 22.97 | 16.35 | 9 | 22074 | 600 | 50582441 |
Musculoskeletal stiffness | 22.68 | 16.35 | 14 | 22069 | 128467 | 50454574 |
Gastrointestinal scarring | 22.64 | 16.35 | 7 | 22076 | 229 | 50582812 |
Thrombocytopenic purpura | 22.63 | 16.35 | 11 | 22072 | 1235 | 50581806 |
Pneumonia | 22.52 | 16.35 | 87 | 21996 | 378314 | 50204727 |
Anaphylactic reaction | 22.51 | 16.35 | 63 | 22020 | 53992 | 50529049 |
Mobility decreased | 22.25 | 16.35 | 4 | 22079 | 79944 | 50503097 |
Condition aggravated | 22.01 | 16.35 | 62 | 22021 | 296996 | 50286045 |
Oropharyngeal discomfort | 21.72 | 16.35 | 16 | 22067 | 3842 | 50579199 |
Exposure during pregnancy | 21.62 | 16.35 | 13 | 22070 | 121002 | 50462039 |
Laryngeal discomfort | 21.36 | 16.35 | 7 | 22076 | 277 | 50582764 |
Sputum abnormal | 21.32 | 16.35 | 8 | 22075 | 474 | 50582567 |
Pain | 21.15 | 16.35 | 157 | 21926 | 578746 | 50004295 |
Antinuclear antibody | 20.94 | 16.35 | 8 | 22075 | 498 | 50582543 |
Balance disorder | 20.83 | 16.35 | 3 | 22080 | 70587 | 50512454 |
Nail infection | 20.43 | 16.35 | 12 | 22071 | 1969 | 50581072 |
Phlebitis | 20.06 | 16.35 | 18 | 22065 | 5702 | 50577339 |
Dysgeusia | 19.93 | 16.35 | 49 | 22034 | 38867 | 50544174 |
Myocardial infarction | 19.88 | 16.35 | 7 | 22076 | 89020 | 50494021 |
Periorbital cellulitis | 19.87 | 16.35 | 8 | 22075 | 573 | 50582468 |
Product dose omission issue | 19.80 | 16.35 | 31 | 22052 | 183807 | 50399234 |
Tumour pain | 19.79 | 16.35 | 10 | 22073 | 1220 | 50581821 |
Chills | 19.67 | 16.35 | 89 | 21994 | 96598 | 50486443 |
Hypermagnesaemia | 19.64 | 16.35 | 9 | 22074 | 885 | 50582156 |
Body temperature abnormal | 19.48 | 16.35 | 10 | 22073 | 1260 | 50581781 |
Infusion site vesicles | 19.05 | 16.35 | 7 | 22076 | 391 | 50582650 |
Hallucination, tactile | 18.80 | 16.35 | 6 | 22077 | 218 | 50582823 |
Influenza | 18.41 | 16.35 | 8 | 22075 | 89530 | 50493511 |
Administration site oedema | 18.29 | 16.35 | 4 | 22079 | 31 | 50583010 |
Cough | 17.81 | 16.35 | 172 | 21911 | 241092 | 50341949 |
Injection site induration | 17.61 | 16.35 | 20 | 22063 | 8377 | 50574664 |
Folliculitis | 17.61 | 16.35 | 47 | 22036 | 39178 | 50543863 |
Onychalgia | 17.45 | 16.35 | 8 | 22075 | 787 | 50582254 |
Drug hypersensitivity | 17.41 | 16.35 | 54 | 22029 | 250956 | 50332085 |
Abdominal operation | 17.27 | 16.35 | 7 | 22076 | 510 | 50582531 |
Muscle injury | 17.20 | 16.35 | 45 | 22038 | 37066 | 50545975 |
Paraesthesia | 17.01 | 16.35 | 100 | 21983 | 120143 | 50462898 |
Cardiotoxicity | 16.93 | 16.35 | 18 | 22065 | 7009 | 50576032 |
Aortitis | 16.75 | 16.35 | 8 | 22075 | 864 | 50582177 |
Toxic encephalopathy | 16.72 | 16.35 | 16 | 22067 | 5499 | 50577542 |
Subacute cutaneous lupus erythematosus | 16.72 | 16.35 | 11 | 22072 | 2204 | 50580837 |
Cardiac failure congestive | 16.63 | 16.35 | 8 | 22075 | 84374 | 50498667 |
Loss of personal independence in daily activities | 16.53 | 16.35 | 5 | 22078 | 70045 | 50512996 |
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 |
---|---|---|---|---|---|---|
Febrile neutropenia | 220.64 | 19.29 | 254 | 12288 | 111986 | 29449999 |
Hiccups | 107.40 | 19.29 | 59 | 12483 | 8794 | 29553191 |
Neutropenia | 102.92 | 19.29 | 193 | 12349 | 131518 | 29430467 |
Hypersensitivity | 99.02 | 19.29 | 117 | 12425 | 52786 | 29509199 |
Erythema | 93.01 | 19.29 | 136 | 12406 | 75470 | 29486515 |
Neutrophil count decreased | 79.26 | 19.29 | 95 | 12447 | 43472 | 29518513 |
Drug ineffective | 78.92 | 19.29 | 28 | 12514 | 363142 | 29198843 |
Nausea | 77.29 | 19.29 | 283 | 12259 | 288972 | 29273013 |
Thrombocytopenia | 65.39 | 19.29 | 163 | 12379 | 134660 | 29427325 |
Stomatitis | 59.55 | 19.29 | 76 | 12466 | 37037 | 29524948 |
Vomiting | 56.79 | 19.29 | 208 | 12334 | 212052 | 29349933 |
Decreased appetite | 54.65 | 19.29 | 160 | 12382 | 145182 | 29416803 |
Fixed eruption | 50.27 | 19.29 | 19 | 12523 | 1183 | 29560802 |
Intestinal ischaemia | 48.40 | 19.29 | 32 | 12510 | 6660 | 29555325 |
Hepatocellular injury | 46.49 | 19.29 | 51 | 12491 | 21192 | 29540793 |
Encephalopathy | 44.26 | 19.29 | 60 | 12482 | 30983 | 29531002 |
Toxicity to various agents | 43.84 | 19.29 | 10 | 12532 | 173651 | 29388334 |
Aplasia | 43.61 | 19.29 | 25 | 12517 | 4038 | 29557947 |
Diarrhoea | 43.11 | 19.29 | 264 | 12278 | 332434 | 29229551 |
Testicular germ cell cancer metastatic | 42.99 | 19.29 | 9 | 12533 | 57 | 29561928 |
Oesophagitis | 41.74 | 19.29 | 37 | 12505 | 11886 | 29550099 |
Mouth ulceration | 40.02 | 19.29 | 34 | 12508 | 10321 | 29551664 |
Anaphylactic reaction | 38.86 | 19.29 | 53 | 12489 | 27520 | 29534465 |
White blood cell count decreased | 38.46 | 19.29 | 99 | 12443 | 83263 | 29478722 |
Stoma site pain | 36.21 | 19.29 | 12 | 12530 | 507 | 29561478 |
Bone marrow failure | 34.58 | 19.29 | 50 | 12492 | 27399 | 29534586 |
Platelet count decreased | 34.39 | 19.29 | 110 | 12432 | 104562 | 29457423 |
Toxic encephalopathy | 33.22 | 19.29 | 22 | 12520 | 4590 | 29557395 |
Sense of oppression | 32.85 | 19.29 | 11 | 12531 | 480 | 29561505 |
Oral pain | 32.81 | 19.29 | 29 | 12513 | 9278 | 29552707 |
Flushing | 32.49 | 19.29 | 50 | 12492 | 28942 | 29533043 |
Febrile bone marrow aplasia | 32.29 | 19.29 | 26 | 12516 | 7325 | 29554660 |
Seminoma | 32.02 | 19.29 | 9 | 12533 | 216 | 29561769 |
Change of bowel habit | 32.00 | 19.29 | 13 | 12529 | 981 | 29561004 |
Mucosal inflammation | 31.97 | 19.29 | 52 | 12490 | 31543 | 29530442 |
Emotional disorder | 31.88 | 19.29 | 22 | 12520 | 4909 | 29557076 |
Interstitial lung disease | 31.34 | 19.29 | 73 | 12469 | 57645 | 29504340 |
Anaphylactic shock | 30.89 | 19.29 | 33 | 12509 | 13303 | 29548682 |
Leukopenia | 30.17 | 19.29 | 70 | 12472 | 55133 | 29506852 |
Enteritis | 29.79 | 19.29 | 24 | 12518 | 6767 | 29555218 |
Peritonitis | 29.71 | 19.29 | 34 | 12508 | 14790 | 29547195 |
Neuropathy peripheral | 29.35 | 19.29 | 81 | 12461 | 70946 | 29491039 |
Pyrexia | 28.05 | 19.29 | 213 | 12329 | 287409 | 29274576 |
Alopecia | 27.36 | 19.29 | 37 | 12505 | 19047 | 29542938 |
Paraesthesia | 25.90 | 19.29 | 65 | 12477 | 53780 | 29508205 |
Regurgitation | 25.46 | 19.29 | 12 | 12530 | 1295 | 29560690 |
Rash maculo-papular | 24.60 | 19.29 | 40 | 12502 | 24249 | 29537736 |
Hypokalaemia | 24.56 | 19.29 | 61 | 12481 | 50142 | 29511843 |
Large intestine perforation | 24.11 | 19.29 | 22 | 12520 | 7334 | 29554651 |
Dehydration | 23.77 | 19.29 | 104 | 12438 | 114644 | 29447341 |
Chemotherapeutic drug level increased | 23.64 | 19.29 | 7 | 12535 | 203 | 29561782 |
Septic shock | 23.55 | 19.29 | 69 | 12473 | 62491 | 29499494 |
Incorrect drug administration rate | 23.53 | 19.29 | 11 | 12531 | 1165 | 29560820 |
Product dose omission issue | 23.41 | 19.29 | 6 | 12536 | 96377 | 29465608 |
Platelet count increased | 23.33 | 19.29 | 23 | 12519 | 8440 | 29553545 |
Jaundice | 22.85 | 19.29 | 43 | 12499 | 29253 | 29532732 |
Acute kidney injury | 20.75 | 19.29 | 187 | 12355 | 265080 | 29296905 |
Oropharyngeal discomfort | 20.39 | 19.29 | 13 | 12529 | 2543 | 29559442 |
Necrotising ulcerative gingivostomatitis | 20.32 | 19.29 | 5 | 12537 | 70 | 29561915 |
Cardiac failure congestive | 20.13 | 19.29 | 4 | 12538 | 76577 | 29485408 |
Hepatic cytolysis | 19.94 | 19.29 | 21 | 12521 | 8326 | 29553659 |
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 |
---|---|---|---|---|---|---|
Febrile neutropenia | 610.87 | 15.29 | 588 | 30272 | 187069 | 64280803 |
Erythema | 231.75 | 15.29 | 360 | 30500 | 186710 | 64281162 |
Nausea | 231.41 | 15.29 | 860 | 30000 | 784940 | 63682932 |
Neutropenia | 227.24 | 15.29 | 409 | 30451 | 239215 | 64228657 |
Mucosal inflammation | 166.01 | 15.29 | 176 | 30684 | 62408 | 64405464 |
Encephalopathy | 153.51 | 15.29 | 164 | 30696 | 58655 | 64409217 |
Drug ineffective | 150.86 | 15.29 | 110 | 30750 | 840137 | 63627735 |
Neutrophil count decreased | 129.83 | 15.29 | 172 | 30688 | 77024 | 64390848 |
Aplasia | 122.74 | 15.29 | 62 | 30798 | 6891 | 64460981 |
Hypersensitivity | 122.40 | 15.29 | 282 | 30578 | 196170 | 64271702 |
Flushing | 118.27 | 15.29 | 166 | 30694 | 78482 | 64389390 |
Febrile bone marrow aplasia | 114.99 | 15.29 | 70 | 30790 | 11185 | 64456687 |
Hiccups | 114.63 | 15.29 | 63 | 30797 | 8313 | 64459559 |
Pyrexia | 103.32 | 15.29 | 533 | 30327 | 558111 | 63909761 |
Hepatocellular injury | 93.88 | 15.29 | 112 | 30748 | 45123 | 64422749 |
Decreased appetite | 93.18 | 15.29 | 321 | 30539 | 280968 | 64186904 |
Bone marrow failure | 90.24 | 15.29 | 113 | 30747 | 47839 | 64420033 |
Stomatitis | 87.37 | 15.29 | 174 | 30686 | 109431 | 64358441 |
Toxicity to various agents | 86.40 | 15.29 | 33 | 30827 | 363480 | 64104392 |
Computerised tomogram thorax abnormal | 85.31 | 15.29 | 33 | 30827 | 1936 | 64465936 |
Neuropathy peripheral | 83.58 | 15.29 | 178 | 30682 | 117347 | 64350525 |
Atelectasis | 81.86 | 15.29 | 82 | 30778 | 27184 | 64440688 |
Sense of oppression | 76.30 | 15.29 | 28 | 30832 | 1419 | 64466453 |
Thrombocytopenia | 72.83 | 15.29 | 254 | 30606 | 223547 | 64244325 |
Fall | 70.13 | 15.29 | 58 | 30802 | 416768 | 64051104 |
Vomiting | 69.58 | 15.29 | 476 | 30384 | 550641 | 63917231 |
Anaphylactic shock | 67.76 | 15.29 | 78 | 30782 | 30250 | 64437622 |
Gastrointestinal disorder | 63.91 | 15.29 | 136 | 30724 | 89573 | 64378299 |
Diarrhoea | 63.55 | 15.29 | 574 | 30286 | 722130 | 63745742 |
Vascular pain | 62.83 | 15.29 | 21 | 30839 | 805 | 64467067 |
Oral pain | 61.91 | 15.29 | 71 | 30789 | 27422 | 64440450 |
Hyponatraemia | 58.68 | 15.29 | 180 | 30680 | 148159 | 64319713 |
Interstitial lung disease | 53.96 | 15.29 | 134 | 30726 | 97598 | 64370274 |
Anaphylactic reaction | 53.47 | 15.29 | 108 | 30752 | 68556 | 64399316 |
Leukopenia | 50.91 | 15.29 | 134 | 30726 | 101108 | 64366764 |
Constipation | 49.44 | 15.29 | 229 | 30631 | 229108 | 64238764 |
Feeling hot | 48.36 | 15.29 | 82 | 30778 | 45581 | 64422291 |
Hypoxia | 47.75 | 15.29 | 120 | 30740 | 88029 | 64379843 |
Palmar-plantar erythrodysaesthesia syndrome | 46.54 | 15.29 | 63 | 30797 | 28756 | 64439116 |
Toxic encephalopathy | 46.17 | 15.29 | 38 | 30822 | 9777 | 64458095 |
Oesophagitis | 45.59 | 15.29 | 54 | 30806 | 21576 | 64446296 |
Infusion site streaking | 44.76 | 15.29 | 14 | 30846 | 433 | 64467439 |
Intestinal ischaemia | 44.72 | 15.29 | 40 | 30820 | 11509 | 64456363 |
Infusion related reaction | 44.52 | 15.29 | 176 | 30684 | 164291 | 64303581 |
Oropharyngeal discomfort | 44.04 | 15.29 | 29 | 30831 | 5306 | 64462566 |
Testicular germ cell cancer metastatic | 42.04 | 15.29 | 9 | 30851 | 56 | 64467816 |
Product dose omission issue | 40.97 | 15.29 | 21 | 30839 | 194726 | 64273146 |
Respiratory syncytial virus infection | 40.31 | 15.29 | 31 | 30829 | 7237 | 64460635 |
Injection site vasculitis | 39.91 | 15.29 | 7 | 30853 | 11 | 64467861 |
Computerised tomogram thorax | 39.05 | 15.29 | 10 | 30850 | 146 | 64467726 |
Chest discomfort | 38.76 | 15.29 | 133 | 30727 | 115973 | 64351899 |
Alopecia | 38.33 | 15.29 | 169 | 30691 | 165521 | 64302351 |
Depression | 38.21 | 15.29 | 20 | 30840 | 183271 | 64284601 |
White blood cell count decreased | 38.05 | 15.29 | 163 | 30697 | 157674 | 64310198 |
Alveolitis | 37.80 | 15.29 | 23 | 30837 | 3669 | 64464203 |
Fixed eruption | 37.37 | 15.29 | 19 | 30841 | 2140 | 64465732 |
Paraesthesia | 37.24 | 15.29 | 145 | 30715 | 134377 | 64333495 |
Platelet count decreased | 35.77 | 15.29 | 167 | 30693 | 167544 | 64300328 |
Rash maculo-papular | 35.46 | 15.29 | 73 | 30787 | 46953 | 64420919 |
Dyspnoea | 35.35 | 15.29 | 510 | 30350 | 718164 | 63749708 |
Asthma | 34.43 | 15.29 | 3 | 30857 | 95222 | 64372650 |
Condition aggravated | 34.28 | 15.29 | 80 | 30780 | 372346 | 64095526 |
Cardiac failure congestive | 34.20 | 15.29 | 10 | 30850 | 130570 | 64337302 |
Overdose | 33.87 | 15.29 | 17 | 30843 | 159549 | 64308323 |
Inappropriate antidiuretic hormone secretion | 33.40 | 15.29 | 47 | 30813 | 22242 | 64445630 |
Seminoma | 32.22 | 15.29 | 9 | 30851 | 186 | 64467686 |
Hypokalaemia | 31.80 | 15.29 | 129 | 30731 | 121774 | 64346098 |
Chemotherapy | 31.25 | 15.29 | 15 | 30845 | 1492 | 64466380 |
Colony stimulating factor therapy | 31.03 | 15.29 | 11 | 30849 | 504 | 64467368 |
Myocardial infarction | 30.48 | 15.29 | 21 | 30839 | 165800 | 64302072 |
Dermatitis acneiform | 30.26 | 15.29 | 28 | 30832 | 8415 | 64459457 |
Mobility decreased | 30.24 | 15.29 | 3 | 30857 | 85837 | 64382035 |
Balance disorder | 29.40 | 15.29 | 3 | 30857 | 83923 | 64383949 |
Injection site phlebitis | 29.12 | 15.29 | 8 | 30852 | 155 | 64467717 |
Hepatic cytolysis | 27.85 | 15.29 | 34 | 30826 | 14015 | 64453857 |
Rheumatoid arthritis | 27.39 | 15.29 | 23 | 30837 | 164271 | 64303601 |
Abdominal pain | 27.21 | 15.29 | 248 | 30612 | 312127 | 64155745 |
Enteritis | 26.87 | 15.29 | 31 | 30829 | 12046 | 64455826 |
Chills | 26.60 | 15.29 | 133 | 30727 | 137131 | 64330741 |
Tonsillar haemorrhage | 25.59 | 15.29 | 8 | 30852 | 247 | 64467625 |
Septic shock | 25.48 | 15.29 | 109 | 30751 | 105328 | 64362544 |
Cholestasis | 25.25 | 15.29 | 62 | 30798 | 44810 | 64423062 |
Musculoskeletal stiffness | 24.86 | 15.29 | 14 | 30846 | 123192 | 64344680 |
Arthritis | 24.71 | 15.29 | 5 | 30855 | 83809 | 64384063 |
Dysgeusia | 24.38 | 15.29 | 63 | 30797 | 46984 | 64420888 |
Intentional product misuse | 24.27 | 15.29 | 3 | 30857 | 72292 | 64395580 |
Neutropenic colitis | 24.23 | 15.29 | 19 | 30841 | 4562 | 64463310 |
Cardiotoxicity | 23.92 | 15.29 | 27 | 30833 | 10247 | 64457625 |
Dental fistula | 23.78 | 15.29 | 9 | 30851 | 497 | 64467375 |
Chronic obstructive pulmonary disease | 23.73 | 15.29 | 3 | 30857 | 71045 | 64396827 |
Periorbital cellulitis | 23.56 | 15.29 | 10 | 30850 | 746 | 64467126 |
Drug clearance decreased | 23.49 | 15.29 | 15 | 30845 | 2604 | 64465268 |
Epistaxis | 23.37 | 15.29 | 101 | 30759 | 98030 | 64369842 |
Dehydration | 23.05 | 15.29 | 180 | 30680 | 216583 | 64251289 |
Folliculitis | 23.04 | 15.29 | 47 | 30813 | 30030 | 64437842 |
Ileus | 22.68 | 15.29 | 40 | 30820 | 22926 | 64444946 |
Muscle injury | 22.28 | 15.29 | 43 | 30817 | 26394 | 64441478 |
Suicidal ideation | 21.77 | 15.29 | 3 | 30857 | 66539 | 64401333 |
Joint swelling | 21.66 | 15.29 | 44 | 30816 | 215338 | 64252534 |
Influenza | 21.64 | 15.29 | 12 | 30848 | 106519 | 64361353 |
Antinuclear antibody | 21.14 | 15.29 | 8 | 30852 | 442 | 64467430 |
Bronchitis | 21.03 | 15.29 | 13 | 30847 | 108730 | 64359142 |
Hyperthermia | 20.69 | 15.29 | 31 | 30829 | 15519 | 64452353 |
Hypomagnesaemia | 20.35 | 15.29 | 51 | 30809 | 37325 | 64430547 |
Nail infection | 20.19 | 15.29 | 12 | 30848 | 1835 | 64466037 |
Anorectal disorder | 19.65 | 15.29 | 12 | 30848 | 1927 | 64465945 |
Intercepted product administration error | 19.62 | 15.29 | 6 | 30854 | 172 | 64467700 |
Chemotherapeutic drug level increased | 19.26 | 15.29 | 7 | 30853 | 345 | 64467527 |
Peritonitis | 19.04 | 15.29 | 39 | 30821 | 24984 | 64442888 |
Malaise | 18.90 | 15.29 | 280 | 30580 | 395967 | 64071905 |
Wrong technique in product usage process | 18.90 | 15.29 | 4 | 30856 | 64970 | 64402902 |
Drug hypersensitivity | 18.86 | 15.29 | 55 | 30805 | 237760 | 64230112 |
Regurgitation | 18.72 | 15.29 | 12 | 30848 | 2097 | 64465775 |
Infusion site vesicles | 18.51 | 15.29 | 7 | 30853 | 386 | 64467486 |
Thrombocytopenic purpura | 18.45 | 15.29 | 12 | 30848 | 2150 | 64465722 |
Keratitis | 18.37 | 15.29 | 14 | 30846 | 3223 | 64464649 |
Osteoarthritis | 18.22 | 15.29 | 4 | 30856 | 63332 | 64404540 |
Loss of personal independence in daily activities | 18.16 | 15.29 | 6 | 30854 | 72448 | 64395424 |
Chronic kidney disease | 18.05 | 15.29 | 3 | 30857 | 57916 | 64409956 |
Administration site oedema | 18.04 | 15.29 | 4 | 30856 | 30 | 64467842 |
Large intestine perforation | 18.03 | 15.29 | 26 | 30834 | 12578 | 64455294 |
Sputum abnormal | 18.00 | 15.29 | 9 | 30851 | 978 | 64466894 |
Disseminated intravascular coagulation | 17.46 | 15.29 | 44 | 30816 | 32304 | 64435568 |
Gait disturbance | 17.45 | 15.29 | 35 | 30825 | 172120 | 64295752 |
Hallucination, tactile | 17.11 | 15.29 | 7 | 30853 | 476 | 64467396 |
Hypermagnesaemia | 17.10 | 15.29 | 9 | 30851 | 1088 | 64466784 |
Aortitis | 17.07 | 15.29 | 9 | 30851 | 1092 | 64466780 |
Hypoglycaemia | 17.03 | 15.29 | 11 | 30849 | 89881 | 64377991 |
Skin reaction | 16.97 | 15.29 | 25 | 30835 | 12327 | 64455545 |
Laryngeal discomfort | 16.89 | 15.29 | 7 | 30853 | 492 | 64467380 |
Heart rate decreased | 16.84 | 15.29 | 3 | 30857 | 55064 | 64412808 |
Cerebellar syndrome | 16.76 | 15.29 | 16 | 30844 | 5000 | 64462872 |
Onychalgia | 16.73 | 15.29 | 8 | 30852 | 789 | 64467083 |
Duodenal ulcer perforation | 16.55 | 15.29 | 45 | 30815 | 34580 | 64433292 |
Body temperature abnormal | 16.48 | 15.29 | 10 | 30850 | 1588 | 64466284 |
Pain | 16.23 | 15.29 | 178 | 30682 | 553333 | 63914539 |
Coombs positive haemolytic anaemia | 16.00 | 15.29 | 8 | 30852 | 870 | 64467002 |
Type III immune complex mediated reaction | 15.92 | 15.29 | 7 | 30853 | 569 | 64467303 |
Palmar erythema | 15.85 | 15.29 | 10 | 30850 | 1700 | 64466172 |
Seizure | 15.79 | 15.29 | 135 | 30725 | 166757 | 64301115 |
Cerebrovascular accident | 15.70 | 15.29 | 26 | 30834 | 137557 | 64330315 |
Influenza like illness | 15.65 | 15.29 | 5 | 30855 | 61697 | 64406175 |
Therapeutic response decreased | 15.62 | 15.29 | 3 | 30857 | 52185 | 64415687 |
Hyperammonaemic encephalopathy | 15.60 | 15.29 | 14 | 30846 | 4044 | 64463828 |
None
Source | Code | Description |
---|---|---|
ATC | A04AD12 | ALIMENTARY TRACT AND METABOLISM ANTIEMETICS AND ANTINAUSEANTS ANTIEMETICS AND ANTINAUSEANTS Other antiemetics |
FDA MoA | N0000010262 | Neurokinin 1 Antagonists |
MeSH PA | D000932 | Antiemetics |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D005765 | Gastrointestinal Agents |
MeSH PA | D064729 | Neurokinin-1 Receptor Antagonists |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D018373 | Peripheral Nervous System Agents |
FDA EPC | N0000175786 | Substance P/Neurokinin-1 Receptor Antagonist |
FDA MoA | N0000182141 | Cytochrome P450 3A4 Inhibitors |
FDA MoA | N0000185506 | Cytochrome P450 3A4 Inducers |
FDA MoA | N0000185507 | Cytochrome P450 2C9 Inducers |
CHEBI has role | CHEBI:35469 | antidepressants |
CHEBI has role | CHEBI:49110 | peripheral nervous system drugs |
CHEBI has role | CHEBI:50919 | antiemetico |
CHEBI has role | CHEBI:55350 | neurokinin-1 receptor antagonists |
CHEBI has role | CHEBI:55351 | substance P receptor antagonists |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Chemotherapy-induced nausea and vomiting | indication | 236084000 | |
Prevention of Post-Operative Nausea and Vomiting | indication | ||
Hepatic failure | contraindication | 59927004 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 8.8 | acidic |
pKa2 | 13.0 | acidic |
pKa3 | 3.22 | Basic |
pKa4 | 2.56 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
125MG | EMEND | MERCK | N021549 | March 26, 2003 | RX | CAPSULE | ORAL | 8258132 | Sept. 26, 2027 | FOR THE PREVENTION OF NAUSEA AND VOMITING ASSOCIATED WITH CHEMOTHERAPY |
125MG | EMEND | MERCK | N021549 | March 26, 2003 | RX | CAPSULE | ORAL | 8258132 | Sept. 26, 2027 | PREVENTION OF POSTOPERATIVE NAUSEA AND VOMITING |
40MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** | EMEND | MERCK | N021549 | June 30, 2006 | DISCN | CAPSULE | ORAL | 8258132 | Sept. 26, 2027 | FOR THE PREVENTION OF NAUSEA AND VOMITING ASSOCIATED WITH CHEMOTHERAPY |
40MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** | EMEND | MERCK | N021549 | June 30, 2006 | DISCN | CAPSULE | ORAL | 8258132 | Sept. 26, 2027 | PREVENTION OF POSTOPERATIVE NAUSEA AND VOMITING |
80MG | EMEND | MERCK | N021549 | March 26, 2003 | RX | CAPSULE | ORAL | 8258132 | Sept. 26, 2027 | FOR THE PREVENTION OF NAUSEA AND VOMITING ASSOCIATED WITH CHEMOTHERAPY |
80MG | EMEND | MERCK | N021549 | March 26, 2003 | RX | CAPSULE | ORAL | 8258132 | Sept. 26, 2027 | PREVENTION OF POSTOPERATIVE NAUSEA AND VOMITING |
125MG/KIT | EMEND | MSD MERCK CO | N207865 | Dec. 17, 2015 | RX | FOR SUSPENSION | ORAL | 8258132 | Sept. 26, 2027 | PREVENTION OF NAUSEA AND VOMITING ASSOCIATED WITH CHEMOTHERAPY (CINV) |
130MG/18ML (7.2MG/ML) | CINVANTI | HERON THERAPS INC | N209296 | Nov. 9, 2017 | RX | EMULSION | INTRAVENOUS | 10624850 | Sept. 18, 2035 | TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY |
130MG/18ML (7.2MG/ML) | CINVANTI | HERON THERAPS INC | N209296 | Nov. 9, 2017 | RX | EMULSION | INTRAVENOUS | 10953018 | Sept. 18, 2035 | TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY |
130MG/18ML (7.2MG/ML) | CINVANTI | HERON THERAPS INC | N209296 | Nov. 9, 2017 | RX | EMULSION | INTRAVENOUS | 9561229 | Sept. 18, 2035 | TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY |
130MG/18ML (7.2MG/ML) | CINVANTI | HERON THERAPS INC | N209296 | Nov. 9, 2017 | RX | EMULSION | INTRAVENOUS | 9808465 | Sept. 18, 2035 | TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY |
130MG/18ML (7.2MG/ML) | CINVANTI | HERON THERAPS INC | N209296 | Nov. 9, 2017 | RX | EMULSION | INTRAVENOUS | 9974794 | Sept. 18, 2035 | TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Substance-P receptor | GPCR | ANTAGONIST | Ki | 10.70 | CHEMBL | CHEMBL | |||
Cytochrome P450 3A4 | Enzyme | WOMBAT-PK | |||||||
Neuromedin-K receptor | GPCR | Ki | 6.34 | CHEMBL | |||||
Substance-P receptor | GPCR | IC50 | 10.05 | CHEMBL |
ID | Source |
---|---|
D02968 | KEGG_DRUG |
357280 | RXNORM |
C1176306 | UMLSCUI |
CHEBI:499361 | CHEBI |
CHEMBL1471 | ChEMBL_ID |
CHEMBL1201782 | ChEMBL_ID |
D000077608 | MESH_DESCRIPTOR_UI |
DB00673 | DRUGBANK_ID |
3490 | IUPHAR_LIGAND_ID |
8050 | INN_ID |
1NF15YR6UY | UNII |
135413536 | PUBCHEM_CID |
17180 | MMSL |
247683 | MMSL |
46392 | MMSL |
d04855 | MMSL |
009926 | NDDF |
4021391 | VANDF |
398690007 | SNOMEDCT_US |
409205009 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0461 | CAPSULE | 80 mg | ORAL | NDA | 31 sections |
EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0461 | CAPSULE | 80 mg | ORAL | NDA | 31 sections |
EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0462 | CAPSULE | 125 mg | ORAL | NDA | 31 sections |
EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0462 | CAPSULE | 125 mg | ORAL | NDA | 31 sections |
EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0464 | CAPSULE | 40 mg | ORAL | NDA | 31 sections |
EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0464 | CAPSULE | 40 mg | ORAL | NDA | 31 sections |
EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3066 | POWDER, FOR SUSPENSION | 125 mg | ORAL | NDA | 31 sections |
EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3066 | POWDER, FOR SUSPENSION | 125 mg | ORAL | NDA | 31 sections |
Aprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-2321 | CAPSULE | 40 mg | ORAL | ANDA | 26 sections |
Aprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-2322 | CAPSULE | 80 mg | ORAL | ANDA | 26 sections |
Aprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-2323 | CAPSULE | 125 mg | ORAL | ANDA | 26 sections |
APREPITANT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13668-591 | CAPSULE | 40 mg | ORAL | ANDA | 25 sections |
APREPITANT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13668-592 | CAPSULE | 80 mg | ORAL | ANDA | 25 sections |
APREPITANT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13668-593 | CAPSULE | 125 mg | ORAL | ANDA | 25 sections |
EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42254-160 | CAPSULE | 40 mg | ORAL | NDA | 26 sections |
CINVANTI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47426-201 | INJECTION, EMULSION | 130 mg | INTRAVENOUS | NDA | 33 sections |
CINVANTI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47426-201 | INJECTION, EMULSION | 130 mg | INTRAVENOUS | NDA | 33 sections |
EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5231 | CAPSULE | 80 mg | ORAL | NDA | 26 sections |
Aprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68462-583 | CAPSULE | 40 mg | ORAL | ANDA | 25 sections |
Aprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68462-584 | CAPSULE | 80 mg | ORAL | ANDA | 25 sections |
Aprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68462-585 | CAPSULE | 125 mg | ORAL | ANDA | 25 sections |