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 | 92.53 | 44.98 | 12 | 431 | 217 | 50604464 |
| Myelopathy | 76.36 | 44.98 | 14 | 429 | 2547 | 50602134 |
| Peripheral motor neuropathy | 50.30 | 44.98 | 9 | 434 | 1422 | 50603259 |
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 |
|---|---|---|---|---|---|---|
| Neuropathy peripheral | 58.99 | 41.64 | 37 | 1228 | 70990 | 29502272 |
| Guillain-Barre syndrome | 48.89 | 41.64 | 15 | 1250 | 5043 | 29568219 |
| Myelopathy | 47.62 | 41.64 | 12 | 1253 | 1962 | 29571300 |
| West Nile viral infection | 43.08 | 41.64 | 9 | 1256 | 641 | 29572621 |
| Peripheral sensory neuropathy | 42.46 | 41.64 | 14 | 1251 | 5925 | 29567337 |
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 | 113.88 | 40.11 | 25 | 1563 | 3949 | 64493195 |
| Subacute combined cord degeneration | 90.06 | 40.11 | 14 | 1574 | 324 | 64496820 |
| Peripheral sensory neuropathy | 70.07 | 40.11 | 21 | 1567 | 11357 | 64485787 |
| Neuropathy peripheral | 68.39 | 40.11 | 40 | 1548 | 117485 | 64379659 |
| Febrile neutropenia | 60.28 | 40.11 | 44 | 1544 | 187613 | 64309531 |
| Muscular weakness | 57.83 | 40.11 | 37 | 1551 | 127301 | 64369843 |
| Neurotoxicity | 55.48 | 40.11 | 22 | 1566 | 27382 | 64469762 |
| Peripheral motor neuropathy | 49.32 | 40.11 | 12 | 1576 | 2958 | 64494186 |
| Polyneuropathy | 47.46 | 40.11 | 18 | 1570 | 19876 | 64477268 |
| West Nile viral infection | 44.94 | 40.11 | 9 | 1579 | 908 | 64496236 |
| Guillain-Barre syndrome | 42.31 | 40.11 | 13 | 1575 | 7622 | 64489522 |
| Hypertriglyceridaemia | 41.31 | 40.11 | 14 | 1574 | 11191 | 64485953 |
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 |
| 38819-10-2 | SECONDARY_CAS_RN |
| 60158CV180 | UNII |
| 135499520 | PUBCHEM_CID |
| 274771 | RXNORM |
| 20608 | MMSL |
| 354214 | MMSL |
| 72483 | MMSL |
| d05655 | MMSL |
| 011068 | NDDF |
| 418538001 | SNOMEDCT_US |
| 418784008 | SNOMEDCT_US |
| C0050203 | UMLSCUI |
| 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 |
| Nelarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70710-1726 | INJECTION | 5 mg | INTRAVENOUS | ANDA | 26 sections |
| Nelarabine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1685 | INJECTION | 5 mg | INTRAVENOUS | ANDA | 1 sections |