Stem definition | Drug id | CAS RN |
---|---|---|
ribofuranyl-derivatives of the "pyrazofurin" type | 667 | 4291-63-8 |
Dose | Unit | Route |
---|---|---|
0.34 | mg | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 18 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.32 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 45 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 7.70 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 14 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.79 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 16 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Feb. 26, 1993 | FDA |
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 |
---|---|---|---|---|---|---|
Lymphopenia | 278.07 | 27.17 | 78 | 2619 | 15543 | 50586884 |
Lymphocyte count decreased | 225.88 | 27.17 | 75 | 2622 | 26232 | 50576195 |
Multiple sclerosis relapse | 189.96 | 27.17 | 75 | 2622 | 42889 | 50559538 |
Leukopenia | 90.91 | 27.17 | 52 | 2645 | 67476 | 50534951 |
Neutropenia | 70.15 | 27.17 | 60 | 2637 | 147905 | 50454522 |
Drug reaction with eosinophilia and systemic symptoms | 58.26 | 27.17 | 29 | 2668 | 28395 | 50574032 |
Febrile neutropenia | 55.41 | 27.17 | 44 | 2653 | 97623 | 50504804 |
Rash maculo-papular | 48.23 | 27.17 | 25 | 2672 | 26616 | 50575811 |
Thrombocytopenia | 45.19 | 27.17 | 44 | 2653 | 127629 | 50474798 |
Abdominal wall wound | 44.93 | 27.17 | 7 | 2690 | 72 | 50602355 |
COVID-19 | 44.85 | 27.17 | 29 | 2668 | 46633 | 50555794 |
Pancytopenia | 43.70 | 27.17 | 36 | 2661 | 83994 | 50518433 |
Myeloblast percentage decreased | 40.70 | 27.17 | 6 | 2691 | 41 | 50602386 |
Intercepted product prescribing error | 39.65 | 27.17 | 7 | 2690 | 161 | 50602266 |
Alanine aminotransferase increased | 36.11 | 27.17 | 33 | 2664 | 88326 | 50514101 |
Gamma-glutamyltransferase increased | 34.99 | 27.17 | 21 | 2676 | 29602 | 50572825 |
Acute myeloid leukaemia recurrent | 34.29 | 27.17 | 9 | 2688 | 1381 | 50601046 |
Refractory cytopenia with multilineage dysplasia | 33.82 | 27.17 | 6 | 2691 | 142 | 50602285 |
Optic neuritis | 30.23 | 27.17 | 12 | 2685 | 6878 | 50595549 |
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 |
---|---|---|---|---|---|---|
Myelodysplastic syndrome | 95.42 | 28.61 | 42 | 2733 | 17752 | 29554000 |
Pancytopenia | 85.50 | 28.61 | 67 | 2708 | 83101 | 29488651 |
Multiple sclerosis relapse | 77.94 | 28.61 | 32 | 2743 | 11387 | 29560365 |
Rash maculo-papular | 68.62 | 28.61 | 37 | 2738 | 24252 | 29547500 |
Febrile neutropenia | 66.22 | 28.61 | 66 | 2709 | 112174 | 29459578 |
Acute generalised exanthematous pustulosis | 53.44 | 28.61 | 20 | 2755 | 5563 | 29566189 |
Lymphopenia | 47.90 | 28.61 | 24 | 2751 | 13509 | 29558243 |
Neutropenia | 47.57 | 28.61 | 60 | 2715 | 131651 | 29440101 |
Face oedema | 44.72 | 28.61 | 21 | 2754 | 10262 | 29561490 |
Leukaemia recurrent | 41.70 | 28.61 | 12 | 2763 | 1465 | 29570287 |
Febrile bone marrow aplasia | 41.46 | 28.61 | 18 | 2757 | 7333 | 29564419 |
Clostridium bacteraemia | 40.06 | 28.61 | 7 | 2768 | 83 | 29571669 |
Toxic skin eruption | 36.58 | 28.61 | 18 | 2757 | 9739 | 29562013 |
Acute erythroid leukaemia | 35.49 | 28.61 | 7 | 2768 | 166 | 29571586 |
Generalised oedema | 34.29 | 28.61 | 18 | 2757 | 11147 | 29560605 |
Herpes zoster | 30.29 | 28.61 | 24 | 2751 | 30028 | 29541724 |
Lymphocyte count decreased | 29.94 | 28.61 | 20 | 2755 | 19251 | 29552501 |
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 |
---|---|---|---|---|---|---|
Lymphopenia | 209.57 | 23.41 | 77 | 4761 | 25580 | 64468314 |
Multiple sclerosis relapse | 167.93 | 23.41 | 75 | 4763 | 41060 | 64452834 |
Lymphocyte count decreased | 131.13 | 23.41 | 63 | 4775 | 40636 | 64453258 |
Febrile neutropenia | 120.94 | 23.41 | 105 | 4733 | 187552 | 64306342 |
Rash maculo-papular | 111.05 | 23.41 | 59 | 4779 | 46967 | 64446927 |
Neutropenia | 109.97 | 23.41 | 111 | 4727 | 239513 | 64254381 |
Pancytopenia | 100.01 | 23.41 | 84 | 4754 | 143225 | 64350669 |
Myelodysplastic syndrome | 86.69 | 23.41 | 42 | 4796 | 27537 | 64466357 |
Leukopenia | 82.49 | 23.41 | 65 | 4773 | 101177 | 64392717 |
Thrombocytopenia | 71.79 | 23.41 | 86 | 4752 | 223715 | 64270179 |
Clostridium bacteraemia | 57.52 | 23.41 | 11 | 4827 | 279 | 64493615 |
Drug reaction with eosinophilia and systemic symptoms | 42.36 | 23.41 | 34 | 4804 | 54183 | 64439711 |
Leukaemia recurrent | 41.84 | 23.41 | 13 | 4825 | 2581 | 64491313 |
Abdominal wall wound | 41.62 | 23.41 | 7 | 4831 | 83 | 64493811 |
Acute generalised exanthematous pustulosis | 39.95 | 23.41 | 20 | 4818 | 14038 | 64479856 |
Myeloblast percentage decreased | 38.64 | 23.41 | 6 | 4832 | 41 | 64493853 |
Acute myeloid leukaemia recurrent | 36.84 | 23.41 | 12 | 4826 | 2772 | 64491122 |
Acute erythroid leukaemia | 34.51 | 23.41 | 7 | 4831 | 242 | 64493652 |
Toxic skin eruption | 31.41 | 23.41 | 19 | 4819 | 19265 | 64474629 |
Product use in unapproved indication | 31.14 | 23.41 | 51 | 4787 | 176567 | 64317327 |
Dermatitis allergic | 30.20 | 23.41 | 17 | 4821 | 15092 | 64478802 |
Stomatococcal infection | 28.61 | 23.41 | 6 | 4832 | 245 | 64493649 |
Peptic ulcer haemorrhage | 25.87 | 23.41 | 7 | 4831 | 854 | 64493040 |
Multiple organ dysfunction syndrome | 24.59 | 23.41 | 34 | 4804 | 101379 | 64392515 |
Herpes zoster | 24.59 | 23.41 | 30 | 4808 | 79157 | 64414737 |
None
Source | Code | Description |
---|---|---|
ATC | L01BB04 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ANTIMETABOLITES Purine analogues |
ATC | L04AA40 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants |
FDA EPC | N0000175712 | Purine Antimetabolite |
CHEBI has role | CHEBI:35610 | antineoplastic agents |
CHEBI has role | CHEBI:35705 | immunosuppressive agents |
MeSH PA | D000970 | Antineoplastic Agents |
MeSH PA | D007155 | Immunologic Factors |
MeSH PA | D007166 | Immunosuppressive Agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Hairy cell leukemia | indication | 118613001 | |
Relapsing remitting multiple sclerosis | indication | 426373005 | DOID:2378 |
Langerhans cell histiocytosis | off-label use | 65399007 | DOID:2571 |
Waldenström macroglobulinemia | off-label use | 190818004 | DOID:0050747 |
Hyperuricemia | contraindication | 35885006 | DOID:1920 |
Kidney disease | contraindication | 90708001 | DOID:557 |
Anemia | contraindication | 271737000 | DOID:2355 |
Pregnancy, function | contraindication | 289908002 | |
Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
Peripheral nerve disease | contraindication | 302226006 | |
Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
Bone marrow depression | contraindication | 307762000 | |
Breastfeeding (mother) | contraindication | 413712001 | |
Uric Acid Nephropathy Gout | contraindication |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 12.14 | acidic |
pKa2 | 13.72 | acidic |
pKa3 | 3.11 | Basic |
pKa4 | 2.3 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
10MG | MAVENCLAD | EMD SERONO INC | N022561 | March 29, 2019 | RX | TABLET | ORAL | 7888328 | April 11, 2024 | TREATMENT OF MS WITH A TABLET WITH AN ADMIXTURE OF (A) AN AMORPHOUS INCLUSION COMPLEX OF CLADRIBINE AND HYDROXYPROPYL-B-CYCLODEXTRIN AND (B) AMORPHOUS FREE CLADRIBINE AND CYCLODEXTRIN AS A NON-INCLUSION COMPLEX, CLADRIBINE/CYCLODEXTRIN 1:10-1:16 W/W |
10MG | MAVENCLAD | EMD SERONO INC | N022561 | March 29, 2019 | RX | TABLET | ORAL | 8785415 | April 11, 2024 | TREATMENT OF MS WITH AN ADMIXTURE OF (A) AN AMORPHOUS INCLUSION COMPLEX OF CLADRIBINE (2CDA) AND CYCLODEXTRIN AND (B) AMORPHOUS FREE 2CDA AND CYCLODEXTRIN AS A NON-INCLUSION COMPLEX, FORMULATED AS A SOLID ORAL FORM, W/O SIGN. AMOUNTS OF CRYST. 2CDA |
10MG | MAVENCLAD | EMD SERONO INC | N022561 | March 29, 2019 | RX | TABLET | ORAL | 8377903 | May 31, 2026 | TREATING RRMS OR SPMS WITH ORAL CLADRIBINE: (I) 2-4 MONTHS INDUCTION WITH 1.7 MG/KG - 3.5 MG/KG CLADRIBINE; (II) CLADRIBINE-FREE PERIOD OF ABOUT 8-10 MONTHS; (III) 2-4 MONTHS MAINTENANCE WITH ABOUT 1.7 MG/KG CLADRIBINE; (IV) CLADRIBINE-FREE PERIOD |
10MG | MAVENCLAD | EMD SERONO INC | N022561 | March 29, 2019 | RX | TABLET | ORAL | 7713947 | Oct. 16, 2026 | TREATING MS WITH ORAL CLADRIBINE ACC. TO THE STEPS (I) INDUCTION PERIOD WITH ABOUT 1.7 MG/KG-3.5 MG/KG CLADRIBINE; (II) CLADRIBINE-FREE PERIOD OF ABOUT 8-10 MONTHS; (III) MAINTENANCE PERIOD WITH ABOUT 1.7 MG/KG CLADRIBINE; (IV) CLADRIBINE-FREE PERIOD |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
10MG | MAVENCLAD | EMD SERONO INC | N022561 | March 29, 2019 | RX | TABLET | ORAL | March 29, 2022 | NEW PRODUCT |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Deoxycytidine kinase | Kinase | WOMBAT-PK | |||||||
cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Enzyme | IC50 | 5.44 | DRUG MATRIX | |||||
Adenosine receptor A1 | GPCR | Ki | 5.14 | CHEMBL | |||||
Adenosine receptor A2a | GPCR | Ki | 4.69 | CHEMBL |
ID | Source |
---|---|
4020629 | VUID |
N0000148293 | NUI |
D01370 | KEGG_DRUG |
2122636 | RXNORM |
4020629 | VANDF |
C0092801 | UMLSCUI |
CHEBI:567361 | CHEBI |
CL9 | PDB_CHEM_ID |
CHEMBL1619 | ChEMBL_ID |
DB00242 | DRUGBANK_ID |
D017338 | MESH_DESCRIPTOR_UI |
20279 | PUBCHEM_CID |
4799 | IUPHAR_LIGAND_ID |
6997 | INN_ID |
47M74X9YT5 | UNII |
1760 | MMSL |
262155 | MMSL |
31821 | MMSL |
4461 | MMSL |
d03001 | MMSL |
004145 | NDDF |
108800000 | SNOMEDCT_US |
386916009 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Cladribine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9871 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 23 sections |
Cladribine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42658-010 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | ANDA | 26 sections |
Mavenclad | HUMAN PRESCRIPTION DRUG LABEL | 1 | 44087-4000 | TABLET | 10 mg | ORAL | NDA | 32 sections |
Cladribine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-140 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 15 sections |
Cladribine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-450 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 23 sections |
Cladribine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-450 | INJECTION | 1 mg | INTRAVENOUS | ANDA | 23 sections |