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 ยตM/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 | 221.01 | 34.57 | 112 | 3073 | 97555 | 50504384 |
Bone marrow failure | 116.69 | 34.57 | 49 | 3136 | 27575 | 50574364 |
Capillary leak syndrome | 93.04 | 34.57 | 22 | 3163 | 1868 | 50600071 |
Multiple organ dysfunction syndrome | 85.95 | 34.57 | 48 | 3137 | 50289 | 50551650 |
Mucosal inflammation | 78.83 | 34.57 | 42 | 3143 | 40100 | 50561839 |
Haematotoxicity | 73.55 | 34.57 | 25 | 3160 | 7870 | 50594069 |
Staphylococcal bacteraemia | 68.11 | 34.57 | 21 | 3164 | 4856 | 50597083 |
Septic shock | 57.74 | 34.57 | 39 | 3146 | 57136 | 50544803 |
Palmar-plantar erythrodysaesthesia syndrome | 57.01 | 34.57 | 27 | 3158 | 20071 | 50581868 |
Blood bilirubin increased | 53.14 | 34.57 | 30 | 3155 | 32008 | 50569931 |
Pyrexia | 51.18 | 34.57 | 88 | 3097 | 380115 | 50221824 |
Pancytopenia | 50.53 | 34.57 | 42 | 3143 | 83988 | 50517951 |
Hyperbilirubinaemia | 47.23 | 34.57 | 19 | 3166 | 9551 | 50592388 |
Transaminases increased | 45.99 | 34.57 | 26 | 3159 | 27798 | 50574141 |
Blood culture positive | 45.50 | 34.57 | 15 | 3170 | 4293 | 50597646 |
Leukaemia recurrent | 43.41 | 34.57 | 11 | 3174 | 1243 | 50600696 |
Neutropenia | 41.92 | 34.57 | 49 | 3136 | 147916 | 50454023 |
Staphylococcal sepsis | 41.88 | 34.57 | 16 | 3169 | 7020 | 50594919 |
Graft versus host disease | 36.62 | 34.57 | 14 | 3171 | 6152 | 50595787 |
Enterobacter bacteraemia | 35.76 | 34.57 | 7 | 3178 | 241 | 50601698 |
Alanine aminotransferase increased | 35.08 | 34.57 | 35 | 3150 | 88324 | 50513615 |
Aspartate aminotransferase increased | 34.91 | 34.57 | 33 | 3152 | 77965 | 50523974 |
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 | 208.13 | 29.37 | 157 | 4421 | 112083 | 29457866 |
Haematotoxicity | 118.40 | 29.37 | 43 | 4535 | 6656 | 29563293 |
Blood bilirubin increased | 117.07 | 29.37 | 70 | 4508 | 33823 | 29536126 |
Capillary leak syndrome | 99.96 | 29.37 | 28 | 4550 | 1871 | 29568078 |
Multiple organ dysfunction syndrome | 98.53 | 29.37 | 80 | 4498 | 63036 | 29506913 |
Palmar-plantar erythrodysaesthesia syndrome | 94.61 | 29.37 | 46 | 4532 | 14713 | 29555236 |
Oedema | 93.69 | 29.37 | 65 | 4513 | 40418 | 29529531 |
Sepsis | 84.71 | 29.37 | 107 | 4471 | 142575 | 29427374 |
Skin toxicity | 77.18 | 29.37 | 27 | 4551 | 3744 | 29566205 |
Aplasia | 75.21 | 29.37 | 27 | 4551 | 4036 | 29565913 |
Mucosal inflammation | 73.69 | 29.37 | 51 | 4527 | 31544 | 29538405 |
Hepatotoxicity | 69.78 | 29.37 | 40 | 4538 | 17827 | 29552122 |
Aspartate aminotransferase increased | 69.40 | 29.37 | 64 | 4514 | 59661 | 29510288 |
Alanine aminotransferase increased | 63.68 | 29.37 | 66 | 4512 | 70878 | 29499071 |
Neutropenia | 58.65 | 29.37 | 86 | 4492 | 131625 | 29438324 |
Cystitis haemorrhagic | 53.15 | 29.37 | 22 | 4556 | 4820 | 29565129 |
Bone marrow failure | 49.63 | 29.37 | 38 | 4540 | 27411 | 29542538 |
Pancytopenia | 48.60 | 29.37 | 62 | 4516 | 83106 | 29486843 |
Pneumonia fungal | 46.22 | 29.37 | 21 | 4557 | 5756 | 29564193 |
Venoocclusive liver disease | 45.62 | 29.37 | 22 | 4556 | 6895 | 29563054 |
Streptococcal sepsis | 45.37 | 29.37 | 14 | 4564 | 1309 | 29568640 |
Adenovirus infection | 41.47 | 29.37 | 18 | 4560 | 4429 | 29565520 |
Transaminases increased | 40.14 | 29.37 | 31 | 4547 | 22631 | 29547318 |
Hyperbilirubinaemia | 36.89 | 29.37 | 25 | 4553 | 14909 | 29555040 |
Acute lymphocytic leukaemia recurrent | 36.56 | 29.37 | 14 | 4564 | 2502 | 29567447 |
Enterococcal bacteraemia | 35.33 | 29.37 | 12 | 4566 | 1521 | 29568428 |
Nephropathy toxic | 33.94 | 29.37 | 21 | 4557 | 10735 | 29559214 |
Tumour lysis syndrome | 33.72 | 29.37 | 23 | 4555 | 13861 | 29556088 |
Staphylococcal infection | 33.25 | 29.37 | 31 | 4547 | 29209 | 29540740 |
Venoocclusive disease | 32.90 | 29.37 | 13 | 4565 | 2526 | 29567423 |
Pulmonary haemorrhage | 31.55 | 29.37 | 19 | 4559 | 9251 | 29560698 |
Blood culture positive | 31.52 | 29.37 | 15 | 4563 | 4562 | 29565387 |
Acute graft versus host disease in skin | 31.25 | 29.37 | 15 | 4563 | 4649 | 29565300 |
Bacterial sepsis | 31.13 | 29.37 | 15 | 4563 | 4688 | 29565261 |
Neutropenic colitis | 30.03 | 29.37 | 12 | 4566 | 2399 | 29567550 |
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 | 344.61 | 28.34 | 227 | 6745 | 187430 | 64304330 |
Haematotoxicity | 178.76 | 28.34 | 63 | 6909 | 12833 | 64478927 |
Blood bilirubin increased | 162.58 | 28.34 | 92 | 6880 | 57461 | 64434299 |
Multiple organ dysfunction syndrome | 162.34 | 28.34 | 113 | 6859 | 101300 | 64390460 |
Capillary leak syndrome | 158.80 | 28.34 | 42 | 6930 | 3255 | 64488505 |
Palmar-plantar erythrodysaesthesia syndrome | 132.83 | 28.34 | 64 | 6908 | 28755 | 64463005 |
Mucosal inflammation | 127.26 | 28.34 | 81 | 6891 | 62503 | 64429257 |
Bone marrow failure | 115.09 | 28.34 | 69 | 6903 | 47883 | 64443877 |
Aplasia | 108.02 | 28.34 | 37 | 6935 | 6916 | 64484844 |
Oedema | 103.49 | 28.34 | 83 | 6889 | 91852 | 64399908 |
Skin toxicity | 94.31 | 28.34 | 33 | 6939 | 6569 | 64485191 |
Aspartate aminotransferase increased | 90.16 | 28.34 | 86 | 6886 | 119702 | 64372058 |
Alanine aminotransferase increased | 88.33 | 28.34 | 91 | 6881 | 138940 | 64352820 |
Sepsis | 88.00 | 28.34 | 116 | 6856 | 230225 | 64261535 |
Neutropenia | 84.40 | 28.34 | 116 | 6856 | 239508 | 64252252 |
Cystitis haemorrhagic | 73.94 | 28.34 | 29 | 6943 | 7927 | 64483833 |
Transaminases increased | 71.93 | 28.34 | 50 | 6922 | 44544 | 64447216 |
Pancytopenia | 70.46 | 28.34 | 82 | 6890 | 143227 | 64348533 |
Hepatotoxicity | 69.64 | 28.34 | 47 | 6925 | 39915 | 64451845 |
Hyperbilirubinaemia | 65.52 | 28.34 | 36 | 6936 | 21169 | 64470591 |
Pyrexia | 61.02 | 28.34 | 164 | 6808 | 558480 | 63933280 |
Pneumonia fungal | 60.79 | 28.34 | 26 | 6946 | 8851 | 64482909 |
Blood culture positive | 60.41 | 28.34 | 25 | 6947 | 7843 | 64483917 |
Venoocclusive liver disease | 57.78 | 28.34 | 26 | 6946 | 9989 | 64481771 |
Fusarium infection | 56.94 | 28.34 | 16 | 6956 | 1553 | 64490207 |
Toxic erythema of chemotherapy | 55.95 | 28.34 | 11 | 6961 | 221 | 64491539 |
Adenovirus infection | 55.53 | 28.34 | 23 | 6949 | 7232 | 64484528 |
Staphylococcal bacteraemia | 53.81 | 28.34 | 25 | 6947 | 10330 | 64481430 |
Acute lymphocytic leukaemia recurrent | 53.21 | 28.34 | 19 | 6953 | 4007 | 64487753 |
Acute myeloid leukaemia recurrent | 51.90 | 28.34 | 17 | 6955 | 2767 | 64488993 |
Staphylococcal infection | 51.18 | 28.34 | 43 | 6929 | 50635 | 64441125 |
Respiratory failure | 50.68 | 28.34 | 74 | 6898 | 161109 | 64330651 |
Venoocclusive disease | 49.64 | 28.34 | 18 | 6954 | 3967 | 64487793 |
Septic shock | 49.57 | 28.34 | 59 | 6913 | 105378 | 64386382 |
Acute graft versus host disease in skin | 43.41 | 28.34 | 19 | 6953 | 6836 | 64484924 |
Aspergillus infection | 43 | 28.34 | 25 | 6947 | 16354 | 64475406 |
Graft versus host disease | 41.42 | 28.34 | 23 | 6949 | 13790 | 64477970 |
Leukaemia recurrent | 41.04 | 28.34 | 14 | 6958 | 2580 | 64489180 |
Fatigue | 39.30 | 28.34 | 16 | 6956 | 748714 | 63743046 |
Bacterial sepsis | 38.74 | 28.34 | 18 | 6954 | 7439 | 64484321 |
Tumour lysis syndrome | 36.59 | 28.34 | 24 | 6948 | 19416 | 64472344 |
Enterococcal infection | 35.96 | 28.34 | 21 | 6951 | 13845 | 64477915 |
Bronchopulmonary aspergillosis | 34.56 | 28.34 | 23 | 6949 | 19062 | 64472698 |
Acute lymphocytic leukaemia | 33.93 | 28.34 | 14 | 6958 | 4357 | 64487403 |
Nephropathy toxic | 33.88 | 28.34 | 22 | 6950 | 17492 | 64474268 |
Enterococcal bacteraemia | 33.78 | 28.34 | 12 | 6960 | 2493 | 64489267 |
Graft versus host disease in skin | 31.21 | 28.34 | 14 | 6958 | 5333 | 64486427 |
Neutropenic colitis | 29.99 | 28.34 | 13 | 6959 | 4568 | 64487192 |
Acute graft versus host disease | 29.65 | 28.34 | 16 | 6956 | 9068 | 64482692 |
None
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 | antineoplastic agents |
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 |
None
None
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 |
---|---|---|---|---|---|---|---|---|---|
Ribonucleoside-diphosphate reductase large subunit | Enzyme | INHIBITOR | IC50 | 8.30 | IUPHAR | CHEMBL | |||
DNA polymerase alpha catalytic subunit | Enzyme | INHIBITOR | WOMBAT-PK | CHEMBL | |||||
Ribonucleoside-diphosphate reductase subunit M2 | Enzyme | INHIBITOR | IC50 | 8.30 | IUPHAR | CHEMBL | |||
Uridine-cytidine kinase 1 | Kinase | WOMBAT-PK | |||||||
cGMP-dependent 3',5'-cyclic phosphodiesterase | Enzyme | IC50 | 5.51 | CHEMBL | |||||
Uridine-cytidine kinase 2 | Kinase | WOMBAT-PK | |||||||
Ribose-phosphate pyrophosphokinase 1 | Kinase | WOMBAT-PK |
ID | Source |
---|---|
4024904 | VUID |
N0000171589 | NUI |
D03546 | KEGG_DRUG |
44151 | RXNORM |
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 |
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 | 16729-431 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 27 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 | 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 |