Stem definition | Drug id | CAS RN |
---|---|---|
4741 | 843663-66-1 |
Dose | Unit | Route |
---|---|---|
86 | mg | O |
None
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 28, 2012 | FDA | JANSSEN THERAP | |
Jan. 19, 2018 | PMDA | Janssen Pharmaceutical KK |
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 |
---|---|---|---|---|---|---|
Electrocardiogram QT prolonged | 409.46 | 32.37 | 139 | 2603 | 51747 | 50550635 |
Hepatotoxicity | 131.62 | 32.37 | 51 | 2691 | 27175 | 50575207 |
Neuropathy peripheral | 120.05 | 32.37 | 71 | 2671 | 96686 | 50505696 |
Intentional product use issue | 102.08 | 32.37 | 59 | 2683 | 76859 | 50525523 |
Anaemia | 96.23 | 32.37 | 91 | 2651 | 252365 | 50350017 |
Off label use | 95.42 | 32.37 | 122 | 2620 | 474304 | 50128078 |
Drug-induced liver injury | 58.13 | 32.37 | 29 | 2713 | 28066 | 50574316 |
Vomiting | 53.79 | 32.37 | 92 | 2650 | 460666 | 50141716 |
Polyneuropathy | 45.64 | 32.37 | 19 | 2723 | 12112 | 50590270 |
Product use in unapproved indication | 44.35 | 32.37 | 42 | 2700 | 115777 | 50486605 |
Meningitis tuberculous | 42.62 | 32.37 | 9 | 2733 | 530 | 50601852 |
Respiratory failure | 40.62 | 32.37 | 36 | 2706 | 91145 | 50511237 |
Aspartate aminotransferase increased | 39.20 | 32.37 | 33 | 2709 | 77965 | 50524417 |
Hypokalaemia | 35.76 | 32.37 | 33 | 2709 | 87959 | 50514423 |
Psychotic disorder | 35.01 | 32.37 | 19 | 2723 | 21793 | 50580589 |
Herbal toxicity | 34.25 | 32.37 | 5 | 2737 | 31 | 50602351 |
Hypomagnesaemia | 33.95 | 32.37 | 19 | 2723 | 23137 | 50579245 |
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 |
---|---|---|---|---|---|---|
Electrocardiogram QT prolonged | 641.53 | 38.30 | 207 | 2753 | 35930 | 29535637 |
Hepatotoxicity | 449.21 | 38.30 | 134 | 2826 | 17733 | 29553834 |
Intentional product use issue | 218.38 | 38.30 | 99 | 2861 | 42399 | 29529168 |
Off label use | 177.73 | 38.30 | 181 | 2779 | 300619 | 29270948 |
Neuropathy peripheral | 170.30 | 38.30 | 99 | 2861 | 70928 | 29500639 |
Anaemia | 79.97 | 38.30 | 99 | 2861 | 200852 | 29370715 |
Optic neuritis | 55.40 | 38.30 | 18 | 2942 | 3091 | 29568476 |
Tuberculosis | 47.26 | 38.30 | 20 | 2940 | 7176 | 29564391 |
Incorrect product administration duration | 47.01 | 38.30 | 17 | 2943 | 4024 | 29567543 |
Drug-induced liver injury | 40.86 | 38.30 | 26 | 2934 | 21629 | 29549938 |
Aspartate aminotransferase increased | 40.31 | 38.30 | 39 | 2921 | 59686 | 29511881 |
Vomiting | 38.81 | 38.30 | 73 | 2887 | 212187 | 29359380 |
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 |
---|---|---|---|---|---|---|
Electrocardiogram QT prolonged | 983.90 | 33.45 | 336 | 5306 | 79112 | 64413978 |
Hepatotoxicity | 543.70 | 33.45 | 182 | 5460 | 39780 | 64453310 |
Intentional product use issue | 305.25 | 33.45 | 154 | 5488 | 95210 | 64397880 |
Neuropathy peripheral | 280.44 | 33.45 | 156 | 5486 | 117369 | 64375721 |
Off label use | 257.45 | 33.45 | 294 | 5348 | 632512 | 63860578 |
Anaemia | 168.41 | 33.45 | 185 | 5457 | 378495 | 64114595 |
Drug-induced liver injury | 86.16 | 33.45 | 53 | 5589 | 47590 | 64445500 |
Vomiting | 82.50 | 33.45 | 161 | 5481 | 550956 | 63942134 |
Aspartate aminotransferase increased | 77.59 | 33.45 | 72 | 5570 | 119716 | 64373374 |
Psychotic disorder | 74.31 | 33.45 | 43 | 5599 | 34535 | 64458555 |
Polyneuropathy | 71.89 | 33.45 | 35 | 5607 | 19859 | 64473231 |
Incorrect product administration duration | 70.65 | 33.45 | 28 | 5614 | 9730 | 64483360 |
Optic neuritis | 64.80 | 33.45 | 25 | 5617 | 8091 | 64484999 |
Product use in unapproved indication | 64.09 | 33.45 | 78 | 5564 | 176540 | 64316550 |
Meningitis tuberculous | 55.70 | 33.45 | 14 | 5628 | 1097 | 64491993 |
Deafness | 53.71 | 33.45 | 28 | 5614 | 18331 | 64474759 |
Tuberculosis | 53.38 | 33.45 | 25 | 5617 | 13013 | 64480077 |
Hypokalaemia | 51.09 | 33.45 | 58 | 5584 | 121845 | 64371245 |
Drug resistance | 50.91 | 33.45 | 34 | 5608 | 35068 | 64458022 |
Myelosuppression | 49.50 | 33.45 | 29 | 5613 | 23801 | 64469289 |
Alanine aminotransferase increased | 48.13 | 33.45 | 60 | 5582 | 138971 | 64354119 |
Respiratory failure | 45.62 | 33.45 | 63 | 5579 | 161120 | 64331970 |
Drug ineffective | 43.91 | 33.45 | 10 | 5632 | 840237 | 63652853 |
Treatment noncompliance | 40.03 | 33.45 | 32 | 5610 | 43450 | 64449640 |
Cardiopulmonary failure | 38.79 | 33.45 | 16 | 5626 | 6154 | 64486936 |
Hypomagnesaemia | 37.63 | 33.45 | 29 | 5613 | 37347 | 64455743 |
Pulmonary tuberculosis | 36.32 | 33.45 | 16 | 5626 | 7228 | 64485862 |
Blood sodium decreased | 34.41 | 33.45 | 25 | 5617 | 29457 | 64463633 |
Optic neuropathy | 34.10 | 33.45 | 12 | 5630 | 2999 | 64490091 |
Pneumothorax | 33.94 | 33.45 | 23 | 5619 | 24275 | 64468815 |
None
Source | Code | Description |
---|---|---|
ATC | J04AK05 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF TUBERCULOSIS Other drugs for treatment of tuberculosis |
FDA CS | M0582947 | Diarylquinolines |
MeSH PA | D000900 | Anti-Bacterial Agents |
MeSH PA | D000890 | Anti-Infective Agents |
MeSH PA | D000995 | Antitubercular Agents |
FDA EPC | N0000186775 | Diarylquinoline Antimycobacterial |
CHEBI has role | CHEBI:33231 | antitubercular agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Pulmonary tuberculosis | indication | 154283005 | DOID:2957 |
Drug resistant tuberculosis | indication | 423709000 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.93 | acidic |
pKa2 | 8.89 | Basic |
pKa3 | 2.19 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
EQ 100MG BASE | SIRTURO | JANSSEN THERAP | N204384 | Dec. 28, 2012 | RX | TABLET | ORAL | 7498343 | Dec. 1, 2026 | TREATMENT OF PULMONARY MULTI-DRUG RESISTANT TUBERCULOSIS |
EQ 20MG BASE | SIRTURO | JANSSEN THERAP | N204384 | May 27, 2020 | RX | TABLET | ORAL | 7498343 | Dec. 1, 2026 | TREATMENT OF PULMONARY MULTI-DRUG RESISTANT TUBERCULOSIS |
EQ 100MG BASE | SIRTURO | JANSSEN THERAP | N204384 | Dec. 28, 2012 | RX | TABLET | ORAL | 8546428 | March 19, 2029 | TREATMENT OF PULMONARY MULTI-DRUG RESISTANT TUBERCULOSIS |
EQ 20MG BASE | SIRTURO | JANSSEN THERAP | N204384 | May 27, 2020 | RX | TABLET | ORAL | 8546428 | March 19, 2029 | TREATMENT OF PULMONARY MULTI-DRUG RESISTANT TUBERCULOSIS |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
EQ 100MG BASE | SIRTURO | JANSSEN THERAP | N204384 | Dec. 28, 2012 | RX | TABLET | ORAL | Aug. 9, 2022 | NEW PATIENT POPULATION |
EQ 100MG BASE | SIRTURO | JANSSEN THERAP | N204384 | Dec. 28, 2012 | RX | TABLET | ORAL | Aug. 9, 2026 | INDICATED AS PART OF COMBINATION THERAPY IN THE TREATMENT OF PEDIATRIC PATIENTS (12 TO LESS THAN 18 YEARS OF AGE AND WEIGHING AT LEAST 30 KG) WITH PULMONARY MULTI-DRUG RESISTANT TUBERCULOSIS |
EQ 100MG BASE | SIRTURO | JANSSEN THERAP | N204384 | Dec. 28, 2012 | RX | TABLET | ORAL | May 27, 2027 | INDICATED AS PART OF COMBINATION THERAPY IN THE TREATMENT OF PEDIATRIC PATIENTS 5 YEARS AND OLDER TO LESS THAN 12 YEARS OF AGE AND WEIGHING AT LEAST 15 KG WITH PULMONARY MULTI-DRUG RESISTANT TUBERCULOSIS (MDR-TB) |
EQ 20MG BASE | SIRTURO | JANSSEN THERAP | N204384 | May 27, 2020 | RX | TABLET | ORAL | May 27, 2027 | INDICATED AS PART OF COMBINATION THERAPY IN THE TREATMENT OF PEDIATRIC PATIENTS 5 YEARS AND OLDER TO LESS THAN 12 YEARS OF AGE AND WEIGHING AT LEAST 15 KG WITH PULMONARY MULTI-DRUG RESISTANT TUBERCULOSIS (MDR-TB) |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 6.43 | CHEMBL | |||||
ATP synthase | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
ATP synthase subunit c | Enzyme | IC50 | 8.60 | CHEMBL | |||||
ATP synthase subunit c | Enzyme | Kd | 6.30 | CHEMBL |
ID | Source |
---|---|
78846I289Y | UNII |
D09872 | KEGG_DRUG |
4032353 | VUID |
N0000187065 | NUI |
845533-86-0 | SECONDARY_CAS_RN |
4032353 | VANDF |
C1664205 | UMLSCUI |
CHEBI:72292 | CHEBI |
BQ1 | PDB_CHEM_ID |
CHEMBL376488 | ChEMBL_ID |
5388906 | PUBCHEM_CID |
DB08903 | DRUGBANK_ID |
CHEMBL2105700 | ChEMBL_ID |
9316 | INN_ID |
C493870 | MESH_SUPPLEMENTAL_RECORD_UI |
11171 | IUPHAR_LIGAND_ID |
1364503 | RXNORM |
196758 | MMSL |
29035 | MMSL |
30320 | MMSL |
d07941 | MMSL |
014821 | NDDF |
014822 | NDDF |
1010553003 | SNOMEDCT_US |
714086004 | SNOMEDCT_US |
714087008 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
SIRTURO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59676-701 | TABLET | 100 mg | ORAL | NDA | 35 sections |
SIRTURO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59676-702 | TABLET | 20 mg | ORAL | NDA | 35 sections |