nelarabine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
arabinofuranosyl derivatives 1892 121032-29-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • nelarabine
  • arranon
  • nelzarabine
  • atriance
prodrug of ara-G
  • Molecular weight: 297.27
  • Formula: C11H15N5O5
  • CLOGP: -0.39
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 4
  • TPSA: 148.77
  • ALOGS: -1.33
  • ROTB: 3
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 2.97 mg/mL Bocci G, Oprea TI, Benet LZ
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:

DateAgencyCompanyOrphan
Aug. 22, 2007 EMA Sandoz Pharmaceuticals d.d.
Oct. 28, 2005 FDA NOVARTIS PHARMS CORP

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Subacute combined cord degeneration 94.41 46.91 12 461 218 63488331
Myelopathy 90.43 46.91 16 457 2810 63485739
Peripheral motor neuropathy 50.30 46.91 9 464 1672 63486877
Sepsis 47.74 46.91 23 450 153100 63335449

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Myelopathy 80.88 40.26 19 1384 2478 34953050
Neuropathy peripheral 55.71 40.26 37 1366 83226 34872302
Peripheral sensory neuropathy 53.71 40.26 17 1386 6743 34948785
Leukoencephalopathy 48.06 40.26 14 1389 4201 34951327
Guillain-Barre syndrome 47.08 40.26 15 1388 6072 34949456
Polyneuropathy 43.99 40.26 18 1385 14878 34940650
West Nile viral infection 42.40 40.26 9 1394 738 34954790
Ataxia 41.80 40.26 17 1386 13836 34941692
Febrile neutropenia 41.37 40.26 38 1365 136811 34818717

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Myelopathy 164.55 41.38 34 1691 4599 79738064
Subacute combined cord degeneration 91.74 41.38 14 1711 327 79742336
Peripheral sensory neuropathy 83.11 41.38 24 1701 13009 79729654
Febrile neutropenia 73.09 41.38 51 1674 230948 79511715
Neurotoxicity 68.75 41.38 26 1699 32492 79710171
Neuropathy peripheral 66.32 41.38 40 1685 141265 79601398
Muscular weakness 54.30 41.38 37 1688 160692 79581971
Polyneuropathy 49.90 41.38 19 1706 24132 79718531
Peripheral motor neuropathy 49.37 41.38 12 1713 3355 79739308
West Nile viral infection 45.31 41.38 9 1716 993 79741670
Ataxia 42.21 41.38 17 1708 25022 79717641
Guillain-Barre syndrome 41.91 41.38 13 1712 8952 79733711

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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)

None

Bioactivity Summary:

None

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 43598-142 INJECTION 5 mg INTRAVENOUS ANDA 28 sections
Nelarabine HUMAN PRESCRIPTION DRUG LABEL 1 70121-1743 INJECTION 5 mg INTRAVENOUS ANDA 28 sections
Nelarabine HUMAN PRESCRIPTION DRUG LABEL 1 70710-1726 INJECTION 5 mg INTRAVENOUS ANDA 26 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
Nelarabine HUMAN PRESCRIPTION DRUG LABEL 1 70771-1685 INJECTION 5 mg INTRAVENOUS ANDA 1 sections
Nelarabine HUMAN PRESCRIPTION DRUG LABEL 1 71288-165 INJECTION 5 mg INTRAVENOUS ANDA 28 sections
NELARABINE HUMAN PRESCRIPTION DRUG LABEL 1 80978-111 INJECTION 250 mg INTRAVENOUS ANDA 19 sections
nelarabine HUMAN PRESCRIPTION DRUG LABEL 1 81927-111 INJECTION 5 mg INTRAVENOUS ANDA 29 sections