nelarabine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| arabinofuranosyl derivatives | 1892 | 121032-29-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
prodrug of ara-G
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 1 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 6.60 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 4.23 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 11 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 4.90 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 81 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.80 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.50 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 28, 2005 | FDA | NOVARTIS PHARMS CORP |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Subacute combined cord degeneration | 93.35 | 47.78 | 12 | 446 | 218 | 56291391 |
| Myelopathy | 83.45 | 47.78 | 15 | 443 | 2633 | 56288976 |
| Peripheral motor neuropathy | 50.25 | 47.78 | 9 | 449 | 1539 | 56290070 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Myelopathy | 66.41 | 43.22 | 16 | 1309 | 2229 | 31693790 |
| Neuropathy peripheral | 57.61 | 43.22 | 37 | 1288 | 75612 | 31620407 |
| Guillain-Barre syndrome | 48.37 | 43.22 | 15 | 1310 | 5345 | 31690674 |
| Peripheral sensory neuropathy | 45.95 | 43.22 | 15 | 1310 | 6300 | 31689719 |
| Polyneuropathy | 45.63 | 43.22 | 18 | 1307 | 13004 | 31683015 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Myelopathy | 141.67 | 41.76 | 30 | 1628 | 4221 | 70922565 |
| Subacute combined cord degeneration | 90.74 | 41.76 | 14 | 1644 | 325 | 70926461 |
| Peripheral sensory neuropathy | 74.19 | 41.76 | 22 | 1636 | 12088 | 70914698 |
| Neuropathy peripheral | 67.45 | 41.76 | 40 | 1618 | 126856 | 70799930 |
| T-cell type acute leukaemia | 63.25 | 41.76 | 10 | 1648 | 273 | 70926513 |
| Neurotoxicity | 61.79 | 41.76 | 24 | 1634 | 29802 | 70896984 |
| Febrile neutropenia | 61.21 | 41.76 | 45 | 1613 | 204273 | 70722513 |
| Muscular weakness | 56.76 | 41.76 | 37 | 1621 | 138299 | 70788487 |
| Polyneuropathy | 50.70 | 41.76 | 19 | 1639 | 21396 | 70905390 |
| Peripheral motor neuropathy | 49.31 | 41.76 | 12 | 1646 | 3120 | 70923666 |
| Precursor T-lymphoblastic lymphoma/leukaemia | 46.90 | 41.76 | 7 | 1651 | 129 | 70926657 |
| West Nile viral infection | 45.19 | 41.76 | 9 | 1649 | 930 | 70925856 |
| Guillain-Barre syndrome | 42.31 | 41.76 | 13 | 1645 | 8027 | 70918759 |
| Ataxia | 42.18 | 41.76 | 17 | 1641 | 23200 | 70903586 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01BB07 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ANTIMETABOLITES Purine analogues |
| FDA MoA | N0000000233 | Nucleic Acid Synthesis Inhibitors |
| FDA EPC | N0000175595 | Nucleoside Metabolic Inhibitor |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:50266 | Prodrugs |
| CHEBI has role | CHEBI:59517 | DNA synthesis inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| T-cell acute lymphoblastic leukemia | indication | 277575008 | |
| Precursor T-cell lymphoblastic lymphoma | indication | 421246008 | |
| Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
| Peripheral demyelinating neuropathy | contraindication | 23414001 | DOID:5214 |
| Demyelination | contraindication | 32693004 | |
| Dehydration | contraindication | 34095006 | |
| Mental handicap | contraindication | 47437004 | |
| Hepatic failure | contraindication | 59927004 | |
| Seizure disorder | contraindication | 128613002 | |
| Intrathecal injection of chemotherapeutic agent | contraindication | 171765004 | |
| Impaired renal function disorder | contraindication | 197663003 | |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Drowsy | contraindication | 271782001 | |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Peripheral nerve disease | contraindication | 302226006 | |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Radiation Therapy of Cranium | contraindication | ||
| Severe Leukopenia | contraindication | ||
| Radiation Therapy of Vertebral Column | contraindication | ||
| Chemotherapy-Induced Hyperuricemia | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.67 | acidic |
| pKa2 | 12.33 | acidic |
| pKa3 | 13.34 | acidic |
| pKa4 | 3.39 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 250MG/50ML (5MG/ML) | NELARABINE | ZYDUS PHARMS | A215037 | Nov. 17, 2021 | RX | INJECTABLE | INTRAVENOUS | May 22, 2022 | COMPETITIVE GENERIC THERAPY |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| 4025093 | VUID |
| N0000175345 | NUI |
| D05134 | KEGG_DRUG |
| 4025093 | VANDF |
| C0907349 | UMLSCUI |
| CHEBI:63612 | CHEBI |
| CHEMBL1201112 | ChEMBL_ID |
| DB01280 | DRUGBANK_ID |
| C104457 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3011155 | PUBCHEM_CID |
| 7090 | IUPHAR_LIGAND_ID |
| 7704 | INN_ID |
| 60158CV180 | UNII |
| 274771 | RXNORM |
| 20608 | MMSL |
| 354214 | MMSL |
| 72483 | MMSL |
| d05655 | MMSL |
| 011068 | NDDF |
| 418538001 | SNOMEDCT_US |
| 418784008 | SNOMEDCT_US |
| C0050203 | UMLSCUI |
| 38819-10-2 | SECONDARY_CAS_RN |
| 135499520 | PUBCHEM_CID |
| 0Z99WX0GPF | UNII |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Arranon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0683 | INJECTION | 5 mg | INTRAVENOUS | NDA | 31 sections |
| Arranon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0683 | INJECTION | 5 mg | INTRAVENOUS | NDA | 31 sections |
| Nelarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70710-1726 | INJECTION | 5 mg | INTRAVENOUS | ANDA | 26 sections |
| Nelarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70710-1839 | INJECTION | 5 mg | INTRAVENOUS | ANDA | 26 sections |
| Nelarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1685 | INJECTION | 5 mg | INTRAVENOUS | ANDA | 1 sections |