Stem definition | Drug id | CAS RN |
---|---|---|
nucleosides antiviral or antineoplastic agents, cytarabine or azacitidine derivatives | 790 | 2353-33-5 |
None
Property | Value | Reference |
---|---|---|
MRTD (Maximum Recommended Therapeutic Daily Dose) | 4.87 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Vd (Volume of distribution) | 4.60 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 130 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 1 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 0.58 hours | Lombardo F, Berellini G, Obach RS |
S (Water solubility) | 10 mg/mL | Bocci G, Oprea TI, Benet LZ |
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Date | Agency | Company | Orphan |
---|---|---|---|
May 2, 2006 | FDA | Astex Pharmaceuticals, Inc. |
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 | 369.34 | 28.96 | 163 | 3385 | 118286 | 63367188 |
Neutropenia | 98.62 | 28.96 | 80 | 3468 | 174925 | 63310549 |
Myelosuppression | 94.44 | 28.96 | 39 | 3509 | 23664 | 63461810 |
Pancytopenia | 92.56 | 28.96 | 61 | 3487 | 96872 | 63388602 |
Bone marrow failure | 89.69 | 28.96 | 40 | 3508 | 29250 | 63456224 |
Pneumonia | 89.41 | 28.96 | 118 | 3430 | 456649 | 63028825 |
Thrombocytopenia | 78.60 | 28.96 | 66 | 3482 | 151091 | 63334383 |
Acute myeloid leukaemia | 74.39 | 28.96 | 30 | 3518 | 17117 | 63468357 |
Acute myeloid leukaemia recurrent | 66.89 | 28.96 | 16 | 3532 | 1607 | 63483867 |
Off label use | 63.65 | 28.96 | 125 | 3423 | 674337 | 62811137 |
Disease progression | 60.48 | 28.96 | 52 | 3496 | 122706 | 63362768 |
Product use in unapproved indication | 59.64 | 28.96 | 61 | 3487 | 179019 | 63306455 |
Sepsis | 52.49 | 28.96 | 53 | 3495 | 153070 | 63332404 |
Pyrexia | 43.93 | 28.96 | 87 | 3461 | 470391 | 63015083 |
Haematotoxicity | 42.72 | 28.96 | 17 | 3531 | 9359 | 63476115 |
Death | 39.53 | 28.96 | 73 | 3475 | 374308 | 63111166 |
Splenic abscess | 39.27 | 28.96 | 7 | 3541 | 162 | 63485312 |
Respiratory failure | 36.22 | 28.96 | 36 | 3512 | 101822 | 63383652 |
Acute myeloid leukaemia refractory | 35.42 | 28.96 | 6 | 3542 | 102 | 63485372 |
Leukaemia recurrent | 34.20 | 28.96 | 9 | 3539 | 1329 | 63484145 |
Escherichia bacteraemia | 32.42 | 28.96 | 11 | 3537 | 3872 | 63481602 |
Pneumonia fungal | 32.40 | 28.96 | 12 | 3536 | 5443 | 63480031 |
Myelodysplastic syndrome | 30.38 | 28.96 | 16 | 3532 | 16738 | 63468736 |
Neutrophil count decreased | 29.99 | 28.96 | 25 | 3523 | 56381 | 63429093 |
Posterior reversible encephalopathy syndrome | 29.86 | 28.96 | 16 | 3532 | 17329 | 63468145 |
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 | 326.76 | 25.21 | 221 | 5070 | 136628 | 34815012 |
Acute myeloid leukaemia | 137.05 | 25.21 | 63 | 5228 | 18207 | 34933433 |
Neutropenia | 117.64 | 25.21 | 131 | 5160 | 156647 | 34794993 |
Off label use | 99.49 | 25.21 | 204 | 5087 | 419320 | 34532320 |
Bone marrow failure | 93.34 | 25.21 | 57 | 5234 | 29196 | 34922444 |
Pancytopenia | 88.02 | 25.21 | 89 | 5202 | 95068 | 34856572 |
Myelosuppression | 86.76 | 25.21 | 47 | 5244 | 19218 | 34932422 |
Infection | 85.86 | 25.21 | 86 | 5205 | 90829 | 34860811 |
Pneumonia | 76.06 | 25.21 | 168 | 5123 | 362459 | 34589181 |
Thrombocytopenia | 71.32 | 25.21 | 102 | 5189 | 156145 | 34795495 |
Sepsis | 67.76 | 25.21 | 103 | 5188 | 166458 | 34785182 |
Acute myeloid leukaemia recurrent | 66.69 | 25.21 | 21 | 5270 | 2149 | 34949491 |
Bacteraemia | 56.73 | 25.21 | 36 | 5255 | 19681 | 34931959 |
Acute myeloid leukaemia refractory | 54.75 | 25.21 | 9 | 5282 | 41 | 34951599 |
Product use in unapproved indication | 48.16 | 25.21 | 73 | 5218 | 117426 | 34834214 |
Aspergillus infection | 41.93 | 25.21 | 25 | 5266 | 12229 | 34939411 |
Pyrexia | 41.33 | 25.21 | 127 | 5164 | 332886 | 34618754 |
Cytopenia | 41.07 | 25.21 | 25 | 5266 | 12698 | 34938942 |
Disease progression | 39.88 | 25.21 | 64 | 5227 | 108013 | 34843627 |
Platelet count decreased | 35.08 | 25.21 | 64 | 5227 | 119653 | 34831987 |
Therapy partial responder | 28.75 | 25.21 | 18 | 5273 | 9598 | 34942042 |
Sinusitis fungal | 28.22 | 25.21 | 8 | 5283 | 570 | 34951070 |
Mucormycosis | 28.13 | 25.21 | 15 | 5276 | 5927 | 34945713 |
Respiratory failure | 28.02 | 25.21 | 55 | 5236 | 108517 | 34843123 |
Anaemia | 27.92 | 25.21 | 88 | 5203 | 233247 | 34718393 |
Drug ineffective | 26.98 | 25.21 | 138 | 5153 | 456613 | 34495027 |
Therapy non-responder | 26.28 | 25.21 | 31 | 5260 | 39115 | 34912525 |
Septal panniculitis | 26.24 | 25.21 | 5 | 5286 | 59 | 34951581 |
Haematotoxicity | 26.18 | 25.21 | 16 | 5275 | 8178 | 34943462 |
Choroidal effusion | 25.98 | 25.21 | 6 | 5285 | 187 | 34951453 |
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 | 661.01 | 25.35 | 365 | 7887 | 230634 | 79505502 |
Neutropenia | 186.05 | 25.35 | 186 | 8066 | 287524 | 79448612 |
Bone marrow failure | 182.28 | 25.35 | 94 | 8158 | 51013 | 79685123 |
Pneumonia | 177.48 | 25.35 | 274 | 7978 | 659972 | 79076164 |
Acute myeloid leukaemia | 174.73 | 25.35 | 78 | 8174 | 30807 | 79705329 |
Myelosuppression | 169.80 | 25.35 | 83 | 8169 | 40213 | 79695923 |
Acute myeloid leukaemia recurrent | 164.33 | 25.35 | 43 | 8209 | 3340 | 79732796 |
Product use in unapproved indication | 142.04 | 25.35 | 151 | 8101 | 250208 | 79485928 |
Pancytopenia | 137.16 | 25.35 | 123 | 8129 | 165622 | 79570514 |
Thrombocytopenia | 133.11 | 25.35 | 150 | 8102 | 265109 | 79471027 |
Sepsis | 124.46 | 25.35 | 146 | 8106 | 269282 | 79466854 |
Off label use | 99.40 | 25.35 | 259 | 7993 | 906956 | 78829180 |
Haematotoxicity | 87.10 | 25.35 | 39 | 8213 | 15480 | 79720656 |
Disease progression | 83.48 | 25.35 | 99 | 8153 | 184263 | 79551873 |
Infection | 82.89 | 25.35 | 113 | 8139 | 241599 | 79494537 |
Acute myeloid leukaemia refractory | 73.93 | 25.35 | 13 | 8239 | 144 | 79735992 |
Bacteraemia | 72.20 | 25.35 | 44 | 8208 | 32780 | 79703356 |
Pyrexia | 64.24 | 25.35 | 184 | 8068 | 678525 | 79057611 |
Aspergillus infection | 59.04 | 25.35 | 32 | 8220 | 19129 | 79717007 |
Leukaemia recurrent | 52.69 | 25.35 | 17 | 8235 | 2757 | 79733379 |
Respiratory failure | 52.25 | 25.35 | 78 | 8174 | 180833 | 79555303 |
Cytopenia | 46.55 | 25.35 | 28 | 8224 | 20355 | 79715781 |
Platelet count decreased | 45.25 | 25.35 | 76 | 8176 | 194588 | 79541548 |
Anaemia | 44.25 | 25.35 | 123 | 8129 | 444892 | 79291244 |
Pneumonia fungal | 43.92 | 25.35 | 22 | 8230 | 11188 | 79724948 |
Therapy partial responder | 37.42 | 25.35 | 23 | 8229 | 17374 | 79718762 |
Mucormycosis | 37.30 | 25.35 | 18 | 8234 | 8451 | 79727685 |
Therapy non-responder | 34.38 | 25.35 | 45 | 8207 | 92260 | 79643876 |
Gene mutation | 33.47 | 25.35 | 12 | 8240 | 2674 | 79733462 |
Cardiac failure | 32.74 | 25.35 | 58 | 8194 | 154784 | 79581352 |
Escherichia bacteraemia | 32.12 | 25.35 | 15 | 8237 | 6547 | 79729589 |
Chronic graft versus host disease | 31.65 | 25.35 | 15 | 8237 | 6766 | 79729370 |
Septic shock | 31.28 | 25.35 | 50 | 8202 | 122751 | 79613385 |
Septal panniculitis | 30.26 | 25.35 | 6 | 8246 | 132 | 79736004 |
Malignant neoplasm progression | 28.82 | 25.35 | 51 | 8201 | 135939 | 79600197 |
Drug ineffective | 27.97 | 25.35 | 199 | 8053 | 1080714 | 78655422 |
Graft versus host disease | 27.65 | 25.35 | 18 | 8234 | 15008 | 79721128 |
Splenic abscess | 26.19 | 25.35 | 7 | 8245 | 589 | 79735547 |
Headache | 25.97 | 25.35 | 18 | 8234 | 653754 | 79082382 |
Delayed engraftment | 25.78 | 25.35 | 6 | 8246 | 286 | 79735850 |
Allogenic stem cell transplantation | 25.72 | 25.35 | 5 | 8247 | 99 | 79736037 |
Bronchopulmonary aspergillosis | 25.52 | 25.35 | 20 | 8232 | 22274 | 79713862 |
None
Source | Code | Description |
---|---|---|
ATC | L01BC08 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ANTIMETABOLITES Pyrimidine analogues |
FDA MoA | N0000000233 | Nucleic Acid Synthesis Inhibitors |
MeSH PA | D000963 | Antimetabolites |
MeSH PA | D000964 | Antimetabolites, Antineoplastic |
MeSH PA | D000970 | Antineoplastic Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D009676 | Noxae |
FDA EPC | N0000175595 | Nucleoside Metabolic Inhibitor |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Acute myeloid leukemia, disease | indication | 91861009 | |
Myelodysplastic syndrome | indication | 109995007 | |
Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
Kidney disease | contraindication | 90708001 | DOID:557 |
Disease of liver | contraindication | 235856003 | DOID:409 |
Pregnancy, function | contraindication | 289908002 | |
Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
Breastfeeding (mother) | contraindication | 413712001 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 12.94 | acidic |
pKa2 | 13.68 | acidic |
pKa3 | 4.39 | Basic |
pKa4 | 2.93 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
100MG;35MG | INQOVI | OTSUKA | N212576 | July 7, 2020 | RX | TABLET | ORAL | 8618075 | Oct. 16, 2028 | METHOD FOR INHIBITING CYTIDINE DEAMINASE BY ADMINISTERING CEDAZURIDINE |
100MG;35MG | INQOVI | OTSUKA | N212576 | July 7, 2020 | RX | TABLET | ORAL | 8618075 | Oct. 16, 2028 | METHOD FOR INHIBITING DEGRADATION OF A CDA SUBSTRATE BY ADMINISTERING CEDAZURIDINE |
100MG;35MG | INQOVI | OTSUKA | N212576 | July 7, 2020 | RX | TABLET | ORAL | 8268800 | Aug. 22, 2030 | METHOD FOR INHIBITING CYTIDINE DEAMINASE BY ADMINISTERING CEDAZURIDINE |
100MG;35MG | INQOVI | OTSUKA | N212576 | July 7, 2020 | RX | TABLET | ORAL | 8268800 | Aug. 22, 2030 | METHOD FOR INHIBITING DEGRADATION OF A CDA SUBSTRATE BY ADMINISTERING CEDAZURIDINE |
100MG;35MG | INQOVI | OTSUKA | N212576 | July 7, 2020 | RX | TABLET | ORAL | 8268800 | Aug. 22, 2030 | TREATMENT OF CHRONIC MYELOMONOCYTIC LEUKEMIA |
100MG;35MG | INQOVI | OTSUKA | N212576 | July 7, 2020 | RX | TABLET | ORAL | 8268800 | Aug. 22, 2030 | TREATMENT OF MYELODYSPLASTIC SYNDROME |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
100MG;35MG | INQOVI | OTSUKA | N212576 | July 7, 2020 | RX | TABLET | ORAL | July 7, 2025 | NEW CHEMICAL ENTITY |
100MG;35MG | INQOVI | OTSUKA | N212576 | July 7, 2020 | RX | TABLET | ORAL | July 7, 2027 | TREATMENT OF ADULT PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS), INCLUDING PREVIOUSLY TREATED AND UNTREATED, DE NOVO AND SECONDARY MDS WITH THE FOLLOWING FRENCH-AMERICAN-BRITISH SUBTYPES (REFRACTORY ANEMIA, REFRACTORY ANEMIA WITH RINGED SIDEROBLASTS, REFRACTORY ANEMIA WITH EXCESS BLASTS, AND CHRONIC MYELOMONOCYTIC LEUKEMIA [CMML]) AND INTERMEDIATE-1, INTERMEDIATE-2, AND HIGH-RISK INTERNATIONAL PROGNOSTIC SCORING SYSTEM GROUPS. |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
DNA (cytosine-5)-methyltransferase 1 | Enzyme | INHIBITOR | IC50 | 7.52 | CHEMBL | CHEMBL | |||
DNA (cytosine-5)-methyltransferase 3A | Enzyme | INHIBITOR | CHEMBL | CHEMBL |
ID | Source |
---|---|
4025438 | VUID |
N0000179023 | NUI |
D03665 | KEGG_DRUG |
879492-57-6 | SECONDARY_CAS_RN |
15657 | RXNORM |
4025438 | VANDF |
C0049065 | UMLSCUI |
CHEBI:50131 | CHEBI |
CHEMBL1201129 | ChEMBL_ID |
DB01262 | DRUGBANK_ID |
D000077209 | MESH_DESCRIPTOR_UI |
451668 | PUBCHEM_CID |
6805 | IUPHAR_LIGAND_ID |
6374 | INN_ID |
776B62CQ27 | UNII |
203877 | MMSL |
21366 | MMSL |
81707 | MMSL |
d05788 | MMSL |
011499 | NDDF |
420517007 | SNOMEDCT_US |
420759005 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9385 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 28 sections |
Decitabine | Human Prescription Drug Label | 1 | 0781-3296 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-749 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 25 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-928 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16729-224 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16729-224 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-231 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 28 sections |
decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-231 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 28 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-348 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-427 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
DECITABINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50742-430 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 24 sections |
DECITABINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50742-430 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 24 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55111-556 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | Human Prescription Drug Label | 1 | 55150-376 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | Human Prescription Drug Label | 1 | 55150-376 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | Human Prescription Drug Label | 1 | 55150-376 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Dacogen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59148-046 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | NDA | 30 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-825 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64679-067 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 24 sections |
INQOVI | HUMAN PRESCRIPTION DRUG LABEL | 2 | 64842-0727 | TABLET, FILM COATED | 35 mg | ORAL | NDA | 31 sections |
INQOVI | HUMAN PRESCRIPTION DRUG LABEL | 2 | 64842-0727 | TABLET, FILM COATED | 35 mg | ORAL | NDA | 31 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67184-0535 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 28 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-316 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68001-422 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
DECITABINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68001-573 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 25 sections |
decitabine | Human Prescription Drug Label | 1 | 68083-528 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-738 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 25 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-285 | INJECTION | 50 mg | INTRAVENOUS | ANDA | 24 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-905 | INJECTION | 50 mg | INTRAVENOUS | ANDA | 21 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-905 | INJECTION | 50 mg | INTRAVENOUS | ANDA | 21 sections |