Stem definition | Drug id | CAS RN |
---|---|---|
arabinofuranosyl derivatives | 691 | 123318-82-1 |
None
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
S (Water solubility) | 1 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 55 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 4.23 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 50 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 1.75 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 7.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.53 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 4 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Nov. 14, 2019 | EMA | ORPHELIA PHARMA SAS | |
Dec. 28, 2004 | FDA | GENZYME |
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 | 238.11 | 33.15 | 128 | 3775 | 94499 | 46587660 |
Bone marrow failure | 156.87 | 33.15 | 67 | 3836 | 29602 | 46652557 |
Multiple organ dysfunction syndrome | 124.22 | 33.15 | 68 | 3835 | 51642 | 46630517 |
Capillary leak syndrome | 122.32 | 33.15 | 29 | 3874 | 1868 | 46680291 |
Acute lymphocytic leukaemia | 101.78 | 33.15 | 27 | 3876 | 2746 | 46679413 |
Mucosal inflammation | 81.94 | 33.15 | 47 | 3856 | 38929 | 46643230 |
Septic shock | 81.40 | 33.15 | 54 | 3849 | 57839 | 46624320 |
Acute myeloid leukaemia | 74.70 | 33.15 | 33 | 3870 | 15745 | 46666414 |
Neutropenia | 69.61 | 33.15 | 72 | 3831 | 143132 | 46539027 |
Acute myeloid leukaemia recurrent | 67.84 | 33.15 | 17 | 3886 | 1379 | 46680780 |
Haematotoxicity | 66.01 | 33.15 | 24 | 3879 | 6909 | 46675250 |
Palmar-plantar erythrodysaesthesia syndrome | 63.57 | 33.15 | 32 | 3871 | 20419 | 46661740 |
Pyrexia | 60.74 | 33.15 | 106 | 3797 | 348696 | 46333463 |
Staphylococcal bacteraemia | 58.21 | 33.15 | 20 | 3883 | 4884 | 46677275 |
Pancytopenia | 54.87 | 33.15 | 50 | 3853 | 85008 | 46597151 |
Bronchopulmonary aspergillosis | 53.43 | 33.15 | 21 | 3882 | 7475 | 46674684 |
Hyperbilirubinaemia | 49.93 | 33.15 | 22 | 3881 | 10416 | 46671743 |
Blood bilirubin increased | 48.27 | 33.15 | 32 | 3871 | 34152 | 46648007 |
Transaminases increased | 46.65 | 33.15 | 29 | 3874 | 27732 | 46654427 |
Enterobacter bacteraemia | 44.93 | 33.15 | 9 | 3894 | 261 | 46681898 |
Respiratory failure | 44.78 | 33.15 | 47 | 3856 | 94769 | 46587390 |
Staphylococcal sepsis | 43.02 | 33.15 | 18 | 3885 | 7514 | 46674645 |
Graft versus host disease | 41.89 | 33.15 | 17 | 3886 | 6571 | 46675588 |
Blood culture positive | 40.65 | 33.15 | 15 | 3888 | 4497 | 46677662 |
Sepsis | 38.63 | 33.15 | 52 | 3851 | 135962 | 46546197 |
Neutropenic sepsis | 37.45 | 33.15 | 19 | 3884 | 12305 | 46669854 |
Toxic erythema of chemotherapy | 37.39 | 33.15 | 6 | 3897 | 46 | 46682113 |
Human herpesvirus 6 infection | 37.12 | 33.15 | 12 | 3891 | 2427 | 46679732 |
Leukaemia recurrent | 35.27 | 33.15 | 10 | 3893 | 1299 | 46680860 |
Thrombocytopenia | 33.83 | 33.15 | 47 | 3856 | 126534 | 46555625 |
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 | 223.70 | 28.00 | 169 | 5088 | 106524 | 29840697 |
Multiple organ dysfunction syndrome | 122.58 | 28.00 | 96 | 5161 | 63391 | 29883830 |
Haematotoxicity | 120.26 | 28.00 | 44 | 5213 | 6126 | 29941095 |
Capillary leak syndrome | 118.53 | 28.00 | 32 | 5225 | 1640 | 29945581 |
Blood bilirubin increased | 113.66 | 28.00 | 74 | 5183 | 36562 | 29910659 |
Sepsis | 110.81 | 28.00 | 132 | 5125 | 146263 | 29800958 |
Palmar-plantar erythrodysaesthesia syndrome | 94.58 | 28.00 | 48 | 5209 | 14822 | 29932399 |
Oedema | 87.19 | 28.00 | 67 | 5190 | 42926 | 29904295 |
Skin toxicity | 81.67 | 28.00 | 28 | 5229 | 3221 | 29944000 |
Neutropenia | 81.24 | 28.00 | 106 | 5151 | 128434 | 29818787 |
Acute lymphocytic leukaemia | 79.27 | 28.00 | 27 | 5230 | 3045 | 29944176 |
Bone marrow failure | 77.55 | 28.00 | 54 | 5203 | 29731 | 29917490 |
Mucosal inflammation | 76.40 | 28.00 | 54 | 5203 | 30440 | 29916781 |
Aplasia | 75.73 | 28.00 | 28 | 5229 | 4009 | 29943212 |
Aspartate aminotransferase increased | 72.03 | 28.00 | 71 | 5186 | 63351 | 29883870 |
Acute myeloid leukaemia recurrent | 66.23 | 28.00 | 20 | 5237 | 1532 | 29945689 |
Alanine aminotransferase increased | 66.14 | 28.00 | 73 | 5184 | 74203 | 29873018 |
Acute myeloid leukaemia | 64.82 | 28.00 | 40 | 5217 | 17966 | 29929255 |
Hepatotoxicity | 64.54 | 28.00 | 40 | 5217 | 18105 | 29929116 |
Cystitis haemorrhagic | 64.14 | 28.00 | 26 | 5231 | 4761 | 29942460 |
Pancytopenia | 62.98 | 28.00 | 76 | 5181 | 84976 | 29862245 |
Respiratory failure | 51.43 | 28.00 | 75 | 5182 | 100567 | 29846654 |
Pneumonia fungal | 47.66 | 28.00 | 22 | 5235 | 5511 | 29941710 |
Streptococcal sepsis | 47.57 | 28.00 | 15 | 5242 | 1327 | 29945894 |
Adenovirus infection | 46.48 | 28.00 | 20 | 5237 | 4248 | 29942973 |
Acute lymphocytic leukaemia recurrent | 44.56 | 28.00 | 17 | 5240 | 2650 | 29944571 |
Neutropenic colitis | 43.79 | 28.00 | 16 | 5241 | 2214 | 29945007 |
Acute graft versus host disease in skin | 42.19 | 28.00 | 19 | 5238 | 4497 | 29942724 |
Transaminases increased | 39.88 | 28.00 | 33 | 5224 | 23424 | 29923797 |
Nephropathy toxic | 39.20 | 28.00 | 24 | 5233 | 10615 | 29936606 |
Enterococcal bacteraemia | 38.71 | 28.00 | 13 | 5244 | 1403 | 29945818 |
Venoocclusive liver disease | 38.13 | 28.00 | 20 | 5237 | 6593 | 29940628 |
Bacterial sepsis | 37.54 | 28.00 | 18 | 5239 | 4908 | 29942313 |
Hyperbilirubinaemia | 35.59 | 28.00 | 27 | 5230 | 16915 | 29930306 |
Neutropenic sepsis | 35.19 | 28.00 | 23 | 5234 | 11386 | 29935835 |
Staphylococcal infection | 34.55 | 28.00 | 34 | 5223 | 30190 | 29917031 |
Pulmonary haemorrhage | 34.12 | 28.00 | 21 | 5236 | 9371 | 29937850 |
Fungal infection | 31.53 | 28.00 | 23 | 5234 | 13577 | 29933644 |
Bronchopulmonary aspergillosis | 31.30 | 28.00 | 22 | 5235 | 12262 | 29934959 |
Tumour lysis syndrome | 30.35 | 28.00 | 22 | 5235 | 12863 | 29934358 |
Blood culture positive | 28.71 | 28.00 | 15 | 5242 | 4904 | 29942317 |
Source | Code | Description |
---|---|---|
ATC | L01BB06 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ANTIMETABOLITES Purine analogues |
FDA MoA | N0000000233 | Nucleic Acid Synthesis Inhibitors |
FDA EPC | N0000175595 | Nucleoside Metabolic Inhibitor |
MeSH PA | D000963 | Antimetabolites |
MeSH PA | D000964 | Antimetabolites, Antineoplastic |
MeSH PA | D000970 | Antineoplastic Agents |
MeSH PA | D009676 | Noxae |
CHEBI has role | CHEBI:35221 | antimetabolite |
CHEBI has role | CHEBI:35610 | cytostatic |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Acute lymphoid leukemia | indication | 91857003 | DOID:9952 |
Mycosis | contraindication | 3218000 | DOID:1564 |
Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
Viral disease | contraindication | 34014006 | DOID:934 |
Dehydration | contraindication | 34095006 | |
Renal failure syndrome | contraindication | 42399005 | DOID:1074 |
Low blood pressure | contraindication | 45007003 | |
Bacterial infectious disease | contraindication | 87628006 | |
Capillary leak syndrome | contraindication | 87730004 | DOID:14400 |
Liver function tests abnormal | contraindication | 166603001 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Sepsis syndrome | contraindication | 238150007 | |
Anemia | contraindication | 271737000 | DOID:2355 |
Pregnancy, function | contraindication | 289908002 | |
Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
Bone marrow depression | contraindication | 307762000 | |
Breastfeeding (mother) | contraindication | 413712001 | |
Chemotherapy-Induced Hyperuricemia | contraindication |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.77 | acidic |
pKa2 | 12.4 | acidic |
pKa3 | 3.11 | Basic |
pKa4 | 2.3 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
DNA polymerase alpha catalytic subunit | Enzyme | INHIBITOR | WOMBAT-PK | CHEMBL | |||||
Ribonucleoside-diphosphate reductase subunit M2 | Enzyme | INHIBITOR | IC50 | 8.30 | IUPHAR | CHEMBL | |||
Ribonucleoside-diphosphate reductase large subunit | Enzyme | INHIBITOR | IC50 | 8.30 | IUPHAR | CHEMBL | |||
Uridine-cytidine kinase 2 | Kinase | WOMBAT-PK | |||||||
Uridine-cytidine kinase 1 | Kinase | WOMBAT-PK | |||||||
Ribose-phosphate pyrophosphokinase 1 | Kinase | WOMBAT-PK |
ID | Source |
---|---|
4024904 | VUID |
N0000171589 | NUI |
D03546 | KEGG_DRUG |
4024904 | VANDF |
C0092777 | UMLSCUI |
CHEBI:681569 | CHEBI |
CFB | PDB_CHEM_ID |
CHEMBL1750 | ChEMBL_ID |
DB00631 | DRUGBANK_ID |
D000077866 | MESH_DESCRIPTOR_UI |
119182 | PUBCHEM_CID |
6802 | IUPHAR_LIGAND_ID |
8422 | INN_ID |
762RDY0Y2H | UNII |
44151 | RXNORM |
19116 | MMSL |
257236 | MMSL |
64071 | MMSL |
d05423 | MMSL |
008803 | NDDF |
413873006 | SNOMEDCT_US |
417601005 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Clolar | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0024-5860 | INJECTION | 1 mg | INTRAVENOUS | NDA | 29 sections |
Clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0955-1746 | INJECTION | 1 mg | INTRAVENOUS | NDA AUTHORIZED GENERIC | 29 sections |
Clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-309 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 23 sections |
CLOFARABINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49315-003 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 1 sections |
CLOFARABINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50742-512 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | ANDA | 23 sections |
Clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-6166 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 26 sections |
CLOFARABINE | Human Prescription Drug Label | 1 | 63323-572 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 24 sections |
clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-546 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 26 sections |
Clofarabine | Human Prescription Drug Label | 1 | 68083-386 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 26 sections |
Clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70121-1236 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 24 sections |
Clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71288-128 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 25 sections |
CLOFARABINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72266-108 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 26 sections |