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 | 229.76 | 33.76 | 115 | 3165 | 105430 | 56183357 |
Bone marrow failure | 126.06 | 33.76 | 51 | 3229 | 28235 | 56260552 |
Capillary leak syndrome | 93.86 | 33.76 | 22 | 3258 | 1944 | 56286843 |
Acute lymphocytic leukaemia | 91.52 | 33.76 | 23 | 3257 | 2721 | 56286066 |
Multiple organ dysfunction syndrome | 87.29 | 33.76 | 48 | 3232 | 52722 | 56236065 |
Mucosal inflammation | 79.33 | 33.76 | 42 | 3238 | 42768 | 56246019 |
Haematotoxicity | 73.97 | 33.76 | 25 | 3255 | 8358 | 56280429 |
Staphylococcal bacteraemia | 68.34 | 33.76 | 21 | 3259 | 5188 | 56283599 |
Septic shock | 58.26 | 33.76 | 39 | 3241 | 60796 | 56227991 |
Palmar-plantar erythrodysaesthesia syndrome | 57.78 | 33.76 | 27 | 3253 | 21038 | 56267749 |
Blood bilirubin increased | 54.17 | 33.76 | 30 | 3250 | 33324 | 56255463 |
Acute myeloid leukaemia | 53.61 | 33.76 | 24 | 3256 | 16948 | 56271839 |
Pyrexia | 52.53 | 33.76 | 90 | 3190 | 418683 | 55870104 |
Pancytopenia | 51.37 | 33.76 | 42 | 3238 | 88673 | 56200114 |
Leukaemia recurrent | 48.63 | 33.76 | 12 | 3268 | 1316 | 56287471 |
Hyperbilirubinaemia | 47.41 | 33.76 | 19 | 3261 | 10216 | 56278571 |
Transaminases increased | 47.05 | 33.76 | 26 | 3254 | 28744 | 56260043 |
Blood culture positive | 46.51 | 33.76 | 15 | 3265 | 4331 | 56284456 |
Staphylococcal sepsis | 42.40 | 33.76 | 16 | 3264 | 7333 | 56281454 |
Neutropenia | 42.33 | 33.76 | 49 | 3231 | 158118 | 56130669 |
Acute myeloid leukaemia recurrent | 37.32 | 33.76 | 10 | 3270 | 1518 | 56287269 |
Sepsis | 36.86 | 33.76 | 43 | 3237 | 139797 | 56148990 |
Graft versus host disease | 36.37 | 33.76 | 14 | 3266 | 6767 | 56282020 |
Enterobacter bacteraemia | 35.81 | 33.76 | 7 | 3273 | 259 | 56288528 |
Alanine aminotransferase increased | 35.63 | 33.76 | 35 | 3245 | 93627 | 56195160 |
Aspartate aminotransferase increased | 35.47 | 33.76 | 33 | 3247 | 82569 | 56206218 |
Respiratory failure | 35.20 | 33.76 | 35 | 3245 | 95027 | 56193760 |
Thrombocytopenia | 34.43 | 33.76 | 41 | 3239 | 136183 | 56152604 |
Venoocclusive liver disease | 34.37 | 33.76 | 12 | 3268 | 4409 | 56284378 |
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 | 211.49 | 28.24 | 161 | 4537 | 121688 | 31570958 |
Haematotoxicity | 117.56 | 28.24 | 43 | 4655 | 7094 | 31685552 |
Blood bilirubin increased | 117.54 | 28.24 | 70 | 4628 | 35066 | 31657580 |
Capillary leak syndrome | 99.55 | 28.24 | 28 | 4670 | 1985 | 31690661 |
Multiple organ dysfunction syndrome | 96.12 | 28.24 | 80 | 4618 | 68123 | 31624523 |
Palmar-plantar erythrodysaesthesia syndrome | 94.41 | 28.24 | 46 | 4652 | 15437 | 31677209 |
Oedema | 93.29 | 28.24 | 65 | 4633 | 42496 | 31650150 |
Sepsis | 84.63 | 28.24 | 108 | 4590 | 151821 | 31540825 |
Acute lymphocytic leukaemia | 80.26 | 28.24 | 27 | 4671 | 3479 | 31689167 |
Skin toxicity | 75.74 | 28.24 | 27 | 4671 | 4132 | 31688514 |
Aplasia | 75.46 | 28.24 | 27 | 4671 | 4176 | 31688470 |
Mucosal inflammation | 71.73 | 28.24 | 51 | 4647 | 34376 | 31658270 |
Hepatotoxicity | 71.53 | 28.24 | 41 | 4657 | 19085 | 31673561 |
Aspartate aminotransferase increased | 69.09 | 28.24 | 64 | 4634 | 62655 | 31629991 |
Alanine aminotransferase increased | 63.26 | 28.24 | 66 | 4632 | 74590 | 31618056 |
Neutropenia | 60.20 | 28.24 | 88 | 4610 | 140276 | 31552370 |
Cystitis haemorrhagic | 52.19 | 28.24 | 22 | 4676 | 5267 | 31687379 |
Acute lymphocytic leukaemia recurrent | 51.80 | 28.24 | 19 | 4679 | 3151 | 31689495 |
Bone marrow failure | 50.41 | 28.24 | 38 | 4660 | 27970 | 31664676 |
Pancytopenia | 48.33 | 28.24 | 62 | 4636 | 87254 | 31605392 |
Streptococcal sepsis | 45.72 | 28.24 | 14 | 4684 | 1333 | 31691313 |
Pneumonia fungal | 45.26 | 28.24 | 21 | 4677 | 6308 | 31686338 |
Venoocclusive liver disease | 45.08 | 28.24 | 22 | 4676 | 7390 | 31685256 |
Adenovirus infection | 41.07 | 28.24 | 18 | 4680 | 4736 | 31687910 |
Acute myeloid leukaemia | 39.64 | 28.24 | 28 | 4670 | 18644 | 31674002 |
Transaminases increased | 39.37 | 28.24 | 31 | 4667 | 24310 | 31668336 |
Enterococcal bacteraemia | 38.62 | 28.24 | 13 | 4685 | 1675 | 31690971 |
Hyperbilirubinaemia | 36.67 | 28.24 | 25 | 4673 | 15725 | 31676921 |
Nephropathy toxic | 33.73 | 28.24 | 21 | 4677 | 11332 | 31681314 |
Staphylococcal infection | 33.17 | 28.24 | 31 | 4667 | 30601 | 31662045 |
Venoocclusive disease | 32.80 | 28.24 | 13 | 4685 | 2659 | 31689987 |
Tumour lysis syndrome | 32.48 | 28.24 | 23 | 4675 | 15362 | 31677284 |
Blood culture positive | 32.08 | 28.24 | 15 | 4683 | 4583 | 31688063 |
Pulmonary haemorrhage | 31.67 | 28.24 | 19 | 4679 | 9596 | 31683050 |
Bacterial sepsis | 31.38 | 28.24 | 15 | 4683 | 4813 | 31687833 |
Acute graft versus host disease in skin | 31.37 | 28.24 | 15 | 4683 | 4817 | 31687829 |
Graft versus host disease in liver | 30.73 | 28.24 | 10 | 4688 | 1160 | 31691486 |
Neutropenic colitis | 29.26 | 28.24 | 12 | 4686 | 2680 | 31689966 |
Respiratory failure | 28.96 | 28.24 | 53 | 4645 | 101396 | 31591250 |
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 | 359.19 | 28.92 | 234 | 6893 | 204084 | 70717233 |
Haematotoxicity | 179.64 | 28.92 | 63 | 7064 | 13611 | 70907706 |
Blood bilirubin increased | 165.41 | 28.92 | 92 | 7035 | 59809 | 70861508 |
Multiple organ dysfunction syndrome | 162.87 | 28.92 | 113 | 7014 | 108402 | 70812915 |
Capillary leak syndrome | 159.80 | 28.92 | 42 | 7085 | 3420 | 70917897 |
Palmar-plantar erythrodysaesthesia syndrome | 134.33 | 28.92 | 64 | 7063 | 30183 | 70891134 |
Acute lymphocytic leukaemia | 131.62 | 28.92 | 40 | 7087 | 5505 | 70915812 |
Mucosal inflammation | 126.68 | 28.92 | 81 | 7046 | 67769 | 70853548 |
Bone marrow failure | 123.69 | 28.92 | 71 | 7056 | 48939 | 70872378 |
Aplasia | 109.14 | 28.92 | 37 | 7090 | 7214 | 70914103 |
Oedema | 100.11 | 28.92 | 83 | 7044 | 103498 | 70817819 |
Sepsis | 93.93 | 28.92 | 119 | 7008 | 244426 | 70676891 |
Skin toxicity | 93.87 | 28.92 | 33 | 7094 | 7165 | 70914152 |
Aspartate aminotransferase increased | 91.24 | 28.92 | 86 | 7041 | 126892 | 70794425 |
Alanine aminotransferase increased | 89.39 | 28.92 | 91 | 7036 | 147389 | 70773928 |
Neutropenia | 87.66 | 28.92 | 118 | 7009 | 257038 | 70664279 |
Acute lymphocytic leukaemia recurrent | 77.65 | 28.92 | 26 | 7101 | 4878 | 70916439 |
Cystitis haemorrhagic | 73.83 | 28.92 | 29 | 7098 | 8564 | 70912753 |
Transaminases increased | 72.83 | 28.92 | 50 | 7077 | 46968 | 70874349 |
Pancytopenia | 71.79 | 28.92 | 82 | 7045 | 151025 | 70770292 |
Hepatotoxicity | 71.04 | 28.92 | 48 | 7079 | 43938 | 70877379 |
Acute myeloid leukaemia | 67.96 | 28.92 | 41 | 7086 | 30899 | 70890418 |
Hyperbilirubinaemia | 65.88 | 28.92 | 36 | 7091 | 22532 | 70898785 |
Venoocclusive liver disease | 64.45 | 28.92 | 28 | 7099 | 10650 | 70910667 |
Blood culture positive | 62 | 28.92 | 25 | 7102 | 7901 | 70913416 |
Pyrexia | 61.99 | 28.92 | 166 | 6961 | 606786 | 70314531 |
Pneumonia fungal | 59.75 | 28.92 | 26 | 7101 | 9927 | 70911390 |
Fusarium infection | 56.53 | 28.92 | 16 | 7111 | 1716 | 70919601 |
Toxic erythema of chemotherapy | 55.85 | 28.92 | 11 | 7116 | 241 | 70921076 |
Adenovirus infection | 55.63 | 28.92 | 23 | 7104 | 7745 | 70913572 |
Acute myeloid leukaemia recurrent | 55.62 | 28.92 | 18 | 7109 | 3036 | 70918281 |
Staphylococcal bacteraemia | 53.94 | 28.92 | 25 | 7102 | 11057 | 70910260 |
Respiratory failure | 52.22 | 28.92 | 74 | 7053 | 168661 | 70752656 |
Staphylococcal infection | 51.95 | 28.92 | 43 | 7084 | 53361 | 70867956 |
Septic shock | 51.73 | 28.92 | 60 | 7067 | 112198 | 70809119 |
Venoocclusive disease | 50.00 | 28.92 | 18 | 7109 | 4182 | 70917135 |
Leukaemia recurrent | 49.09 | 28.92 | 16 | 7111 | 2759 | 70918558 |
Aspergillus infection | 45.33 | 28.92 | 26 | 7101 | 17842 | 70903475 |
Acute graft versus host disease in skin | 44.00 | 28.92 | 19 | 7108 | 7118 | 70914199 |
Graft versus host disease | 41.19 | 28.92 | 23 | 7104 | 15000 | 70906317 |
Fatigue | 40.84 | 28.92 | 16 | 7111 | 824303 | 70097014 |
Bacterial sepsis | 39.56 | 28.92 | 18 | 7109 | 7629 | 70913688 |
Enterococcal bacteraemia | 37.46 | 28.92 | 13 | 7114 | 2713 | 70918604 |
Enterococcal infection | 36.41 | 28.92 | 21 | 7106 | 14561 | 70906756 |
Tumour lysis syndrome | 36.12 | 28.92 | 24 | 7103 | 21336 | 70899981 |
Nephropathy toxic | 34.24 | 28.92 | 22 | 7105 | 18492 | 70902825 |
Bronchopulmonary aspergillosis | 34.08 | 28.92 | 23 | 7104 | 20979 | 70900338 |
Graft versus host disease in skin | 31.50 | 28.92 | 14 | 7113 | 5616 | 70915701 |
Acute graft versus host disease | 29.98 | 28.92 | 16 | 7111 | 9546 | 70911771 |
Neutropenic colitis | 29.53 | 28.92 | 13 | 7114 | 5101 | 70916216 |
Acute lymphocytic leukaemia refractory | 29.33 | 28.92 | 6 | 7121 | 160 | 70921157 |
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 |
---|---|---|---|---|---|---|---|---|---|
DNA polymerase alpha catalytic subunit | Enzyme | INHIBITOR | WOMBAT-PK | CHEMBL | |||||
Ribonucleoside-diphosphate reductase large subunit | Enzyme | INHIBITOR | IC50 | 8.30 | IUPHAR | CHEMBL | |||
Ribonucleoside-diphosphate reductase subunit M2 | Enzyme | INHIBITOR | IC50 | 8.30 | IUPHAR | CHEMBL | |||
Ribose-phosphate pyrophosphokinase 1 | Kinase | WOMBAT-PK | |||||||
Uridine-cytidine kinase 1 | Kinase | WOMBAT-PK | |||||||
Uridine-cytidine kinase 2 | Kinase | WOMBAT-PK | |||||||
cGMP-dependent 3',5'-cyclic phosphodiesterase | Enzyme | IC50 | 5.51 | CHEMBL |
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 | 30 sections |
Clolar | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0024-5860 | INJECTION | 1 mg | INTRAVENOUS | NDA | 30 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 | 24 sections |
Clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-309 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 24 sections |
CLOFARABINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49315-003 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 1 sections |
CLOFARABINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49315-003 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 1 sections |
CLOFARABINE | Human Prescription Drug Label | 1 | 55150-326 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 26 sections |
Clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-6166 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 27 sections |
Clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-6166 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 27 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 | 27 sections |
clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-546 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 27 sections |
Clofarabine | Human Prescription Drug Label | 1 | 68083-386 | 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 | 25 sections |
Clofarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70121-1236 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 25 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 |
CLOFARABINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72266-108 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 26 sections |