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 |
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 | 295.51 | 31.20 | 131 | 2656 | 97536 | 50504801 |
Neutropenia | 87.22 | 31.20 | 69 | 2718 | 147896 | 50454441 |
Bone marrow failure | 82.83 | 31.20 | 37 | 2750 | 27587 | 50574750 |
Pneumonia | 82.03 | 31.20 | 102 | 2685 | 378299 | 50224038 |
Acute myeloid leukaemia | 67.97 | 31.20 | 27 | 2760 | 15047 | 50587290 |
Thrombocytopenia | 59.44 | 31.20 | 52 | 2735 | 127621 | 50474716 |
Pancytopenia | 57.75 | 31.20 | 43 | 2744 | 83987 | 50518350 |
Acute myeloid leukaemia recurrent | 53.86 | 31.20 | 13 | 2774 | 1377 | 50600960 |
Sepsis | 51.79 | 31.20 | 49 | 2738 | 132876 | 50469461 |
Off label use | 48.18 | 31.20 | 90 | 2697 | 474336 | 50128001 |
Haematotoxicity | 45.81 | 31.20 | 17 | 2770 | 7878 | 50594459 |
Pyrexia | 38.34 | 31.20 | 72 | 2715 | 380131 | 50222206 |
Product use in unapproved indication | 38.19 | 31.20 | 39 | 2748 | 115780 | 50486557 |
Myelosuppression | 36.97 | 31.20 | 17 | 2770 | 13500 | 50588837 |
Splenic abscess | 35.91 | 31.20 | 6 | 2781 | 95 | 50602242 |
Myelodysplastic syndrome | 32.15 | 31.20 | 16 | 2771 | 15116 | 50587221 |
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 | 281.46 | 26.42 | 183 | 4054 | 112057 | 29458233 |
Acute myeloid leukaemia | 127.09 | 26.42 | 57 | 4180 | 16456 | 29553834 |
Neutropenia | 93.25 | 26.42 | 104 | 4133 | 131607 | 29438683 |
Bone marrow failure | 89.07 | 26.42 | 53 | 4184 | 27396 | 29542894 |
Pneumonia | 72.49 | 26.42 | 148 | 4089 | 320024 | 29250266 |
Pancytopenia | 69.86 | 26.42 | 72 | 4165 | 83096 | 29487194 |
Off label use | 62.10 | 26.42 | 134 | 4103 | 300666 | 29269624 |
Infection | 56.54 | 26.42 | 62 | 4175 | 76689 | 29493601 |
Sepsis | 48.65 | 26.42 | 79 | 4158 | 142603 | 29427687 |
Acute myeloid leukaemia recurrent | 46.40 | 26.42 | 15 | 4222 | 1765 | 29568525 |
Acute myeloid leukaemia refractory | 45.52 | 26.42 | 7 | 4230 | 20 | 29570270 |
Product use in unapproved indication | 45.52 | 26.42 | 59 | 4178 | 86816 | 29483474 |
Aspergillus infection | 41.12 | 26.42 | 23 | 4214 | 10558 | 29559732 |
Myelosuppression | 38.03 | 26.42 | 23 | 4214 | 12204 | 29558086 |
Pyrexia | 37.80 | 26.42 | 108 | 4129 | 287514 | 29282776 |
Thrombocytopenia | 35.92 | 26.42 | 67 | 4170 | 134756 | 29435534 |
Platelet count decreased | 35.67 | 26.42 | 58 | 4179 | 104614 | 29465676 |
Respiratory failure | 29.32 | 26.42 | 51 | 4186 | 97080 | 29473210 |
Mucormycosis | 27.94 | 26.42 | 14 | 4223 | 5144 | 29565146 |
Choroidal effusion | 27.70 | 26.42 | 6 | 4231 | 147 | 29570143 |
Bacteraemia | 27.48 | 26.42 | 21 | 4216 | 16302 | 29553988 |
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 | 541.41 | 26.96 | 297 | 6306 | 187360 | 64304769 |
Bone marrow failure | 168.53 | 26.96 | 87 | 6516 | 47865 | 64444264 |
Pneumonia | 163.68 | 26.96 | 240 | 6363 | 559336 | 63932793 |
Acute myeloid leukaemia | 154.97 | 26.96 | 69 | 6534 | 27394 | 64464735 |
Neutropenia | 149.17 | 26.96 | 151 | 6452 | 239473 | 64252656 |
Acute myeloid leukaemia recurrent | 133.75 | 26.96 | 35 | 6568 | 2749 | 64489380 |
Product use in unapproved indication | 116.56 | 26.96 | 115 | 6488 | 176503 | 64315626 |
Sepsis | 101.18 | 26.96 | 121 | 6482 | 230220 | 64261909 |
Pancytopenia | 90.19 | 26.96 | 91 | 6512 | 143218 | 64348911 |
Haematotoxicity | 87.74 | 26.96 | 37 | 6566 | 12859 | 64479270 |
Thrombocytopenia | 75.22 | 26.96 | 103 | 6500 | 223698 | 64268431 |
Off label use | 73.95 | 26.96 | 184 | 6419 | 632622 | 63859507 |
Myelosuppression | 68.88 | 26.96 | 38 | 6565 | 23792 | 64468337 |
Infection | 58.94 | 26.96 | 83 | 6520 | 184797 | 64307332 |
Aspergillus infection | 55.40 | 26.96 | 29 | 6574 | 16350 | 64475779 |
Pyrexia | 53.47 | 26.96 | 151 | 6452 | 558493 | 63933636 |
Acute myeloid leukaemia refractory | 49.52 | 26.96 | 8 | 6595 | 51 | 64492078 |
Platelet count decreased | 48.61 | 26.96 | 72 | 6531 | 167639 | 64324490 |
Respiratory failure | 46.43 | 26.96 | 69 | 6534 | 161114 | 64331015 |
Leukaemia recurrent | 45.79 | 26.96 | 15 | 6588 | 2579 | 64489550 |
Bacteraemia | 37.43 | 26.96 | 27 | 6576 | 26884 | 64465245 |
Mucormycosis | 36.79 | 26.96 | 17 | 6586 | 7324 | 64484805 |
Gene mutation | 36.59 | 26.96 | 12 | 6591 | 2070 | 64490059 |
Cardiac failure | 34.33 | 26.96 | 54 | 6549 | 132319 | 64359810 |
Anaemia | 33.81 | 26.96 | 100 | 6503 | 378580 | 64113549 |
Pneumonia fungal | 33.72 | 26.96 | 17 | 6586 | 8860 | 64483269 |
Chronic graft versus host disease | 32.92 | 26.96 | 15 | 6588 | 6261 | 64485868 |
Disease progression | 31.61 | 26.96 | 54 | 6549 | 141626 | 64350503 |
Organising pneumonia | 27.70 | 26.96 | 15 | 6588 | 9040 | 64483089 |
None
Source | Code | Description |
---|---|---|
ATC | L01BC08 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ANTIMETABOLITES Pyrimidine 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 | D004791 | Enzyme Inhibitors |
MeSH PA | D009676 | Noxae |
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 |
6374 | INN_ID |
6805 | IUPHAR_LIGAND_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 | 27 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 | 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 |
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 | 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 | 69539-115 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70121-1644 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 28 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70860-219 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 28 sections |
Decitabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71288-119 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | Human Prescription Drug Label | 1 | 72205-031 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |
Decitabine | Human Prescription Drug Label | 1 | 72205-036 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 27 sections |