sapropterin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
pteridine derivatives 2612 62989-33-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sapropterin hydrochloride
  • tetrahydrobiopterin
  • sapropterin
  • sapropterin dihydrochloride
  • kuvan
  • sapropterin HCl
  • Molecular weight: 241.25
  • Formula: C9H15N5O3
  • CLOGP: -0.77
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 6
  • TPSA: 132
  • ALOGS: -2.07
  • ROTB: 2
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ
S (Water solubility) 2 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP3K21,MAPK7,NTRK2,PDK1,PDK2,PRKDC,TEK 19
kinase-selectivity-class AXL,GRK2,MAP2K6,MAP3K14,MAP3K21,MAPK7,TEK 7
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Dec. 2, 2008 EMA
Dec. 13, 2007 FDA BIOMARIN PHARM

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
Amino acid level increased 368.43 41.15 47 1328 410 90626662
Maternal exposure during pregnancy 190.64 41.15 97 1278 359966 90267106
Abortion spontaneous 71.95 41.15 28 1347 54028 90573044
Product prescribing error 67.75 41.15 23 1352 30122 90596950
Amino acid level decreased 61.61 41.15 8 1367 80 90626992
Anxiety 42.36 41.15 36 1339 309736 90317336
Psychomotor hyperactivity 41.89 41.15 13 1362 12800 90614272

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
Amino acid level increased 186.32 45.13 27 818 486 42620004
Product prescribing error 61.28 45.13 22 823 26090 42594400
Amino acid level decreased 54.03 45.13 8 837 166 42620324

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
Amino acid level increased 140.80 41.18 21 1242 815 110587221
Maternal exposure during pregnancy 119.67 41.18 58 1205 254825 110333211
Product prescribing error 73.44 41.18 26 1237 51305 110536731
Abortion spontaneous 63.19 41.18 21 1242 34261 110553775
Product dose omission issue 54.92 41.18 38 1225 321744 110266292
Amino acid level decreased 48.38 41.18 6 1257 55 110587981
Overdose 43.12 41.18 29 1234 233765 110354271

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A16AX07 ALIMENTARY TRACT AND METABOLISM
OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS
OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS
Various alimentary tract and metabolism products
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000190482 Phenylalanine Hydroxylase Activators
FDA EPC N0000190483 Phenylalanine Hydroxylase Activator
CHEBI has role CHEBI:23354 coenzyme
CHEBI has role CHEBI:33295 diagnostic agent
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:75835 anti-anaemic agent
CHEBI has role CHEBI:23357 cofactor
CHEBI has role CHEBI:50177 dermatologic drug
CHEBI has role CHEBI:62868 hepatoprotective agent
CHEBI has role CHEBI:77746 human metabolite
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

A16AX Various alimentary tract and metabolism products 23 drugs
anethole trithionedoxecitinedoxribtimineeliglustatfosdenopteringivosiranglycerol phenylbutyratelonafarniblumasiranmigalastatmiglustatnedosiran show all 23 →

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Classical phenylketonuria indication 7573000
Tetrahydrobiopterin deficiency indication 68724006
Neutropenic disorder contraindication 303011007 DOID:1227




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.23 acidic
pKa2 5.42 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Phenylalanine-4-hydroxylase Enzyme ACTIVATOR Ki 5.40 IUPHAR CHEMBL
Nitric oxide synthase, brain Enzyme Kd 5.95 CHEMBL

External reference:

IDSource
4027166 VUID
N0000176128 NUI
D01798 KEGG_DRUG
69056-38-8 SECONDARY_CAS_RN
4027166 VANDF
4027167 VANDF
C0048897 UMLSCUI
CHEBI:59560 CHEBI
THB PDB_CHEM_ID
CHEMBL1201774 ChEMBL_ID
CHEMBL1201775 ChEMBL_ID
DB00360 DRUGBANK_ID
C003402 MESH_SUPPLEMENTAL_RECORD_UI
5276 IUPHAR_LIGAND_ID
6553 INN_ID
EGX657432I UNII
135398654 PUBCHEM_CID
751628 RXNORM
129793 MMSL
24913 MMSL
339312 MMSL
d07068 MMSL
007099 NDDF
012473 NDDF
012474 NDDF
432857000 SNOMEDCT_US
432859002 SNOMEDCT_US
434239009 SNOMEDCT_US
EGX657432I INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
sapropterin dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0906 TABLET 100 mg ORAL ANDA 29 sections
sapropterin dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 31722-045 TABLET 100 mg ORAL ANDA 25 sections
Sapropterin dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 31722-047 POWDER, FOR SOLUTION 100 mg ORAL ANDA 26 sections
Sapropterin dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 31722-048 POWDER, FOR SOLUTION 500 mg ORAL ANDA 26 sections
Sapropterin Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42571-509 POWDER, FOR SOLUTION 100 mg ORAL ANDA 25 sections
Sapropterin Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42571-510 POWDER, FOR SOLUTION 500 mg ORAL ANDA 25 sections
JAVYGTOR HUMAN PRESCRIPTION DRUG LABEL 1 43598-096 TABLET 100 mg ORAL ANDA 25 sections
JAVYGTOR HUMAN PRESCRIPTION DRUG LABEL 1 43598-097 POWDER, FOR SOLUTION 100 mg ORAL ANDA 25 sections
JAVYGTOR HUMAN PRESCRIPTION DRUG LABEL 1 43598-162 POWDER, FOR SOLUTION 500 mg ORAL ANDA 25 sections
sapropterin dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 49884-720 TABLET 100 mg ORAL ANDA 22 sections
SAPROPTERIN DIHYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 49884-873 POWDER, FOR SOLUTION 500 mg ORAL ANDA 26 sections
SAPROPTERIN DIHYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 49884-948 POWDER, FOR SOLUTION 100 mg ORAL ANDA 27 sections
Sapropterin Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 52817-850 POWDER, FOR SOLUTION 100 mg ORAL ANDA 19 sections
Sapropterin Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 52817-851 POWDER, FOR SOLUTION 500 mg ORAL ANDA 19 sections
Sapropterin Dihydrochloride Human Prescription Drug Label 1 59651-574 TABLET 100 mg ORAL ANDA 26 sections
Kuvan HUMAN PRESCRIPTION DRUG LABEL 1 68135-300 TABLET 100 mg ORAL NDA 27 sections
Kuvan HUMAN PRESCRIPTION DRUG LABEL 1 68135-301 POWDER, FOR SOLUTION 100 mg ORAL NDA 27 sections
Kuvan HUMAN PRESCRIPTION DRUG LABEL 1 68135-482 POWDER, FOR SOLUTION 500 mg ORAL NDA 27 sections
sapropterin dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 72603-191 TABLET 100 mg ORAL ANDA 25 sections
Sapropterin dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 72603-193 POWDER, FOR SOLUTION 100 mg ORAL ANDA 26 sections
Sapropterin dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 72603-194 POWDER, FOR SOLUTION 500 mg ORAL ANDA 26 sections
ZELVYSIA HUMAN PRESCRIPTION DRUG LABEL 1 73289-0070 POWDER, FOR SOLUTION 100 mg ORAL ANDA 27 sections
ZELVYSIA HUMAN PRESCRIPTION DRUG LABEL 1 73289-0071 POWDER, FOR SOLUTION 500 mg ORAL ANDA 27 sections