Stem definition | Drug id | CAS RN |
---|---|---|
uracil type antineoplastics | 4893 | 183204-74-2 |
None
None
Date | Agency | Company | Orphan |
---|---|---|---|
Sept. 22, 2015 | FDA | TAIHO ONCOLOGY INC | |
March 24, 2014 | PMDA | Taiho Pharmaceutical Co., Ltd. |
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 |
---|---|---|---|---|---|---|
Disease progression | 1044.31 | 36.89 | 368 | 4055 | 101552 | 53243091 |
Death | 644.23 | 36.89 | 384 | 4039 | 356848 | 52987795 |
Nausea | 202.63 | 36.89 | 277 | 4146 | 755814 | 52588829 |
Fatigue | 175.06 | 36.89 | 254 | 4169 | 730252 | 52614391 |
Diarrhoea | 139.89 | 36.89 | 211 | 4212 | 625335 | 52719308 |
Decreased appetite | 129.79 | 36.89 | 121 | 4302 | 214853 | 53129790 |
Vomiting | 106.86 | 36.89 | 165 | 4258 | 496974 | 52847669 |
White blood cell count decreased | 100.96 | 36.89 | 83 | 4340 | 124392 | 53220251 |
Cytopenia | 77.45 | 36.89 | 29 | 4394 | 9141 | 53335502 |
Abdominal pain | 53.26 | 36.89 | 84 | 4339 | 255819 | 53088824 |
Neutropenia | 52.14 | 36.89 | 65 | 4358 | 159120 | 53185523 |
Intestinal obstruction | 43.45 | 36.89 | 28 | 4395 | 28713 | 53315930 |
Inappropriate schedule of product administration | 42.74 | 36.89 | 41 | 4382 | 74837 | 53269806 |
Malignant neoplasm progression | 40.51 | 36.89 | 39 | 4384 | 71502 | 53273141 |
Dysgeusia | 37.59 | 36.89 | 30 | 4393 | 42901 | 53301742 |
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 |
---|---|---|---|---|---|---|
Disease progression | 1261.98 | 34.52 | 496 | 5272 | 86366 | 32421392 |
Death | 735.95 | 34.52 | 571 | 5197 | 381946 | 32125812 |
Fatigue | 327.73 | 34.52 | 352 | 5416 | 350349 | 32157409 |
Nausea | 195.53 | 34.52 | 260 | 5508 | 320589 | 32187169 |
Diarrhoea | 182.66 | 34.52 | 269 | 5499 | 364533 | 32143225 |
Decreased appetite | 145.93 | 34.52 | 160 | 5608 | 160653 | 32347105 |
White blood cell count decreased | 95.29 | 34.52 | 98 | 5670 | 91100 | 32416658 |
Blood alkaline phosphatase abnormal | 62.93 | 34.52 | 15 | 5753 | 457 | 32507301 |
Neutropenia | 56.63 | 34.52 | 95 | 5673 | 142080 | 32365678 |
Colorectal cancer metastatic | 54.48 | 34.52 | 16 | 5752 | 1101 | 32506657 |
Vomiting | 51.06 | 34.52 | 122 | 5646 | 235435 | 32272323 |
Abdominal pain | 50.58 | 34.52 | 93 | 5675 | 149436 | 32358322 |
Intestinal obstruction | 47.52 | 34.52 | 35 | 5733 | 20763 | 32486995 |
Dysgeusia | 47.45 | 34.52 | 38 | 5730 | 25493 | 32482265 |
Malignant neoplasm progression | 46.23 | 34.52 | 63 | 5705 | 78433 | 32429325 |
Cytopenia | 42.81 | 34.52 | 25 | 5743 | 10039 | 32497719 |
Carcinoembryonic antigen increased | 42.33 | 34.52 | 12 | 5756 | 728 | 32507030 |
Therapy cessation | 38.96 | 34.52 | 28 | 5740 | 15985 | 32491773 |
Alopecia | 38.83 | 34.52 | 31 | 5737 | 20699 | 32487059 |
Stoma site haemorrhage | 38.32 | 34.52 | 12 | 5756 | 1026 | 32506732 |
Blood count abnormal | 37.06 | 34.52 | 25 | 5743 | 12901 | 32494857 |
Anaemia | 36.27 | 34.52 | 104 | 5664 | 223520 | 32284238 |
Source | Code | Description |
---|---|---|
FDA MoA | N0000191869 | Thymidine Phosphorylase Inhibitors |
FDA EPC | N0000191870 | Thymidine Phosphorylase Inhibitor |
CHEBI has role | CHEBI:35610 | cytostatic |
CHEBI has role | CHEBI:90878 | EC 2.4.2.4 inhibitor |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Malignant tumor of stomach | indication | 363349007 | DOID:10534 |
Malignant tumor of colon | indication | 363406005 | DOID:219 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 7.78 | acidic |
pKa2 | 9.98 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | RE46284 | Sept. 22, 2029 | TREATMENT OF ADULTS WITH METASTATIC GASTRIC OR GJA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY THAT INCLUDED A FLUOROPYRIMIDINE, A PLATINUM, EITHER A TAXANE OR IRINOTECAN, AND IF APPROPIATE, HER2/NEU-TARGETED THERAPY |
EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | RE46284 | Sept. 22, 2029 | TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN- AND IRINOTECAN-BASED CHEMOTHERAPY, AN ANTI-VEGF BIOLOGICAL THERAPY, AND IF RAS WILD-TYPE, AN ANTI-EGFR THERAPY |
EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | RE46284 | Sept. 22, 2029 | TREATMENT OF ADULTS WITH METASTATIC GASTRIC OR GJA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY THAT INCLUDED A FLUOROPYRIMIDINE, A PLATINUM, EITHER A TAXANE OR IRINOTECAN, AND IF APPROPIATE, HER2/NEU-TARGETED THERAPY |
EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | RE46284 | Sept. 22, 2029 | TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN- AND IRINOTECAN-BASED CHEMOTHERAPY, AN ANTI-VEGF BIOLOGICAL THERAPY, AND IF RAS WILD-TYPE, AN ANTI-EGFR THERAPY |
EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | 10456399 | Feb. 3, 2037 | METHOD OF TREATING CANCER BY DETECTING A CREATININE CLEARANCE OF A PATIENT AND ADMINISTERING LONSURF |
EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | 10960004 | Feb. 3, 2037 | METHOD OF TREATING CANCER BY DETECTING A CREATININE CLEARANCE OF A PATIENT AND ADMINISTERING LONSURF |
EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | 10456399 | Feb. 3, 2037 | METHOD OF TREATING CANCER BY DETECTING A CREATININE CLEARANCE OF A PATIENT AND ADMINISTERING LONSURF |
EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | 10960004 | Feb. 3, 2037 | METHOD OF TREATING CANCER BY DETECTING A CREATININE CLEARANCE OF A PATIENT AND ADMINISTERING LONSURF |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | Feb. 22, 2022 | TREATMENT OF ADULT PATIENTS WITH METASTATIC GASTRIC OR GASTROESOPHAGEAL JUNCTION ADENOCARCINOMA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY |
EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | Feb. 22, 2022 | TREATMENT OF ADULT PATIENTS WITH METASTATIC GASTRIC OR GASTROESOPHAGEAL JUNCTION ADENOCARCINOMA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY |
EQ 6.14MG BASE;15MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | Feb. 22, 2026 | TREATMENT OF ADULT PATIENTS WITH METASTATIC GASTRIC OR GASTROESOPHAGEAL JUNCTION ADENOCARCINOMA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY |
EQ 8.19MG BASE;20MG | LONSURF | TAIHO ONCOLOGY | N207981 | Sept. 22, 2015 | RX | TABLET | ORAL | Feb. 22, 2026 | TREATMENT OF ADULT PATIENTS WITH METASTATIC GASTRIC OR GASTROESOPHAGEAL JUNCTION ADENOCARCINOMA PREVIOUSLY TREATED WITH AT LEAST TWO PRIOR LINES OF CHEMOTHERAPY, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Thymidine phosphorylase | Enzyme | INHIBITOR | IC50 | 7.70 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Thymidine phosphorylase | Enzyme | IC50 | 7.70 | CHEMBL |
ID | Source |
---|---|
NGO10K751P | UNII |
D10467 | KEGG_DRUG |
183204-72-0 | SECONDARY_CAS_RN |
4034880 | VANDF |
C4056441 | UMLSCUI |
CHEBI:90879 | CHEBI |
CMU | PDB_CHEM_ID |
CHEMBL235668 | ChEMBL_ID |
6323266 | PUBCHEM_CID |
DB09343 | DRUGBANK_ID |
CHEMBL65375 | ChEMBL_ID |
C000613754 | MESH_SUPPLEMENTAL_RECORD_UI |
8696 | IUPHAR_LIGAND_ID |
9500 | INN_ID |
1670303 | RXNORM |
31200 | MMSL |
d08381 | MMSL |
016454 | NDDF |
016455 | NDDF |
724029008 | SNOMEDCT_US |
724030003 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
LONSURF | HUMAN PRESCRIPTION DRUG LABEL | 2 | 64842-1020 | TABLET, FILM COATED | 8.19 mg | ORAL | NDA | 27 sections |
LONSURF | HUMAN PRESCRIPTION DRUG LABEL | 2 | 64842-1025 | TABLET, FILM COATED | 6.14 mg | ORAL | NDA | 27 sections |