Stem definition | Drug id | CAS RN |
---|---|---|
1944 | 104206-65-7 |
Dose | Unit | Route |
---|---|---|
20 | mg | O |
Property | Value | Reference |
---|---|---|
MRTD (Maximum Recommended Therapeutic Daily Dose) | 6.07 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 90 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Date | Agency | Company | Orphan |
---|---|---|---|
Feb. 21, 2005 | EMA | Swedish Orphan Biovitrum International AB | |
Jan. 18, 2002 | FDA | SWEDISH ORPHAN |
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 |
---|---|---|---|---|---|---|
Amino acid level increased | 283.03 | 117.79 | 32 | 246 | 296 | 50604550 |
Succinylacetone increased | 155.93 | 117.79 | 14 | 264 | 0 | 50604846 |
Alpha 1 foetoprotein increased | 130.59 | 117.79 | 15 | 263 | 156 | 50604690 |
Liver transplant | 129.61 | 117.79 | 20 | 258 | 2112 | 50602734 |
Hepatocellular carcinoma | 123.34 | 117.79 | 19 | 259 | 1980 | 50602866 |
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 |
---|---|---|---|---|---|---|
Amino acid level increased | 399.19 | 79.71 | 48 | 328 | 315 | 29573836 |
Liver transplant | 200.24 | 79.71 | 33 | 343 | 2283 | 29571868 |
Lenticular opacities | 159.85 | 79.71 | 20 | 356 | 181 | 29573970 |
Succinylacetone increased | 123.47 | 79.71 | 12 | 364 | 0 | 29574151 |
Alpha 1 foetoprotein increased | 90.78 | 79.71 | 14 | 362 | 617 | 29573534 |
Hepatocellular carcinoma | 88.82 | 79.71 | 20 | 356 | 7018 | 29567133 |
Cataract | 88.01 | 79.71 | 25 | 351 | 22353 | 29551798 |
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 |
---|---|---|---|---|---|---|
Amino acid level increased | 644.11 | 80.67 | 75 | 511 | 530 | 64497616 |
Liver transplant | 312.43 | 80.67 | 50 | 536 | 4042 | 64494104 |
Lenticular opacities | 274.35 | 80.67 | 34 | 552 | 410 | 64497736 |
Alpha 1 foetoprotein increased | 181.07 | 80.67 | 25 | 561 | 715 | 64497431 |
Cataract | 162.89 | 80.67 | 45 | 541 | 51217 | 64446929 |
Hepatocellular carcinoma | 162.19 | 80.67 | 32 | 554 | 8371 | 64489775 |
Succinylacetone increased | 148.69 | 80.67 | 14 | 572 | 0 | 64498146 |
None
Source | Code | Description |
---|---|---|
ATC | A16AX04 | ALIMENTARY TRACT AND METABOLISM OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS Various alimentary tract and metabolism products |
MeSH PA | D004791 | Enzyme Inhibitors |
FDA MoA | N0000175808 | Hydroxyphenylpyruvate Dioxygenase Inhibitors |
FDA EPC | N0000175809 | 4-Hydroxyphenyl-Pyruvate Dioxygenase Inhibitor |
FDA MoA | N0000185504 | Cytochrome P450 2C9 Inhibitors |
FDA MoA | N0000190110 | Organic Anion Transporter 1 Inhibitors |
FDA MoA | N0000190111 | Organic Anion Transporter 3 Inhibitors |
FDA MoA | N0000193955 | Cytochrome P450 2E1 Inducers |
CHEBI has role | CHEBI:38317 | HPPD inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Tyrosinemia type I | indication | 410056006 | |
Hypophosphatemia | contraindication | 4996001 | |
Pain in eye | contraindication | 41652007 | |
Hypertyrosinemia | contraindication | 56595005 | |
Red eye | contraindication | 75705005 | |
Leukopenia | contraindication | 84828003 | DOID:615 |
Kidney disease | contraindication | 90708001 | DOID:557 |
Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
Photophobia | contraindication | 409668002 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 3.5 | acidic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
4MG/ML | ORFADIN | SWEDISH ORPHAN | N206356 | April 22, 2016 | RX | SUSPENSION | ORAL | 9301932 | Feb. 28, 2033 | TREATMENT OF HEREDITARY TYROSINEMIA TYPE 1 (HT-1) IN COMBINATION WITH DIETARY RESTRICTION OF TYROSINE AND PHENYLALANINE |
10MG | NITYR | CYCLE PHARMS LTD | N209449 | July 26, 2017 | RX | TABLET | ORAL | 10328029 | Jan. 5, 2035 | TREATMENT OF HEREDITARY TYROSINEMIA TYPE 1 (HT-1) IN COMBINATION WITH DIETARY RESTRICTION OF TYROSINE AND PHENYLALANINE |
2MG | NITYR | CYCLE PHARMS LTD | N209449 | July 26, 2017 | RX | TABLET | ORAL | 10328029 | Jan. 5, 2035 | TREATMENT OF HEREDITARY TYROSINEMIA TYPE 1 (HT-1) IN COMBINATION WITH DIETARY RESTRICTION OF TYROSINE AND PHENYLALANINE |
5MG | NITYR | CYCLE PHARMS LTD | N209449 | July 26, 2017 | RX | TABLET | ORAL | 10328029 | Jan. 5, 2035 | TREATMENT OF HEREDITARY TYROSINEMIA TYPE 1 (HT-1) IN COMBINATION WITH DIETARY RESTRICTION OF TYROSINE AND PHENYLALANINE |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
4-hydroxyphenylpyruvate dioxygenase | Enzyme | INHIBITOR | IC50 | 7.40 | WOMBAT-PK | CHEMBL | |||
4-hydroxyphenylpyruvate dioxygenase | Enzyme | IC50 | 7.40 | CHEMBL | |||||
4-hydroxyphenylpyruvate dioxygenase | Unclassified | IC50 | 7.40 | CHEMBL |
ID | Source |
---|---|
4021290 | VUID |
N0000148727 | NUI |
D05177 | KEGG_DRUG |
4021290 | VANDF |
C0173083 | UMLSCUI |
CHEBI:50378 | CHEBI |
CHEMBL1337 | ChEMBL_ID |
DB00348 | DRUGBANK_ID |
C077073 | MESH_SUPPLEMENTAL_RECORD_UI |
115355 | PUBCHEM_CID |
6834 | IUPHAR_LIGAND_ID |
7720 | INN_ID |
K5BN214699 | UNII |
326381 | RXNORM |
16303 | MMSL |
251189 | MMSL |
42739 | MMSL |
d04789 | MMSL |
009172 | NDDF |
009558 | NDDF |
385996000 | SNOMEDCT_US |
385997009 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0254-3020 | CAPSULE | 2 mg | ORAL | ANDA | 26 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0254-3021 | CAPSULE | 5 mg | ORAL | ANDA | 26 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0254-3022 | CAPSULE | 10 mg | ORAL | ANDA | 26 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-2233 | CAPSULE | 10 mg | ORAL | ANDA | 26 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-2233 | CAPSULE | 10 mg | ORAL | ANDA | 26 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-2234 | CAPSULE | 2 mg | ORAL | ANDA | 26 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-2234 | CAPSULE | 2 mg | ORAL | ANDA | 26 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-2235 | CAPSULE | 5 mg | ORAL | ANDA | 26 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-2235 | CAPSULE | 5 mg | ORAL | ANDA | 26 sections |
Orfadin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66658-102 | CAPSULE | 2 mg | ORAL | NDA | 27 sections |
Orfadin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66658-102 | CAPSULE | 2 mg | ORAL | NDA | 27 sections |
Orfadin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66658-105 | CAPSULE | 5 mg | ORAL | NDA | 27 sections |
Orfadin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66658-105 | CAPSULE | 5 mg | ORAL | NDA | 27 sections |
Orfadin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66658-110 | CAPSULE | 10 mg | ORAL | NDA | 27 sections |
Orfadin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66658-110 | CAPSULE | 10 mg | ORAL | NDA | 27 sections |
Orfadin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66658-120 | CAPSULE | 20 mg | ORAL | NDA | 27 sections |
Orfadin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66658-120 | CAPSULE | 20 mg | ORAL | NDA | 27 sections |
ORFADIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66658-204 | SUSPENSION | 4 mg | ORAL | NDA | 27 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70505-202 | CAPSULE | 2 mg | ORAL | ANDA | 27 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70505-205 | CAPSULE | 5 mg | ORAL | ANDA | 27 sections |
Nitisinone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70505-210 | CAPSULE | 10 mg | ORAL | ANDA | 27 sections |
NITYR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70709-000 | TABLET | 10 mg | ORAL | NDA | 27 sections |
NITYR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70709-002 | TABLET | 2 mg | ORAL | NDA | 27 sections |
NITYR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70709-005 | TABLET | 5 mg | ORAL | NDA | 27 sections |