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nateglinide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihyperglycaemics | 1886 | 105816-04-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.36 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.32 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 13 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 16.20 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 73 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.15 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.03 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.50 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.862 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 5.188 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 15.524 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 5.715 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.860 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.400 | % | High | 1 |
| herg | hERG pIC50 | 4.810 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 5.754 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 9.863 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.740 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK,TGFBR1 | 21 | |||
| kinase-selectivity-class | EIF2AK3,GRK2 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.855 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 29.376 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.710 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.916 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.250 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 29.107 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 50 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 1.230 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 972.747 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 22, 2000 | FDA | NOVARTIS |
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 |
|---|---|---|---|---|---|---|
| Lactic acidosis | 75.79 | 26.62 | 28 | 1252 | 50435 | 90576732 |
| Blood glucose increased | 46.70 | 26.62 | 24 | 1256 | 95222 | 90531945 |
| Glycosylated haemoglobin increased | 32.31 | 26.62 | 11 | 1269 | 15551 | 90611616 |
| Hypoglycaemia | 26.89 | 26.62 | 15 | 1265 | 69833 | 90557334 |
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 |
|---|---|---|---|---|---|---|
| Hypoglycaemia | 22.95 | 22.22 | 17 | 1274 | 59837 | 42560207 |
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 |
|---|---|---|---|---|---|---|
| Lactic acidosis | 58.09 | 22.18 | 31 | 2199 | 92780 | 110494289 |
| Hypoglycaemia | 54.22 | 22.18 | 32 | 2198 | 116072 | 110470997 |
| Blood glucose increased | 35.95 | 22.18 | 26 | 2204 | 132470 | 110454599 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BX03 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Other blood glucose lowering drugs, excl. insulins |
| FDA EPC | N0000175428 | Glinide |
| FDA MoA | N0000175448 | Potassium Channel Antagonists |
| MeSH PA | D007004 | Hypoglycemic Agents |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:68612 | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor |
Related Drugs by ATC class:
A10BX Other blood glucose lowering drugs, excl. insulins 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diabetes mellitus type 2 | indication | 44054006 | DOID:9352 |
| Infectious disease | contraindication | 40733004 | |
| Hypopituitarism | contraindication | 74728003 | DOID:9406 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Hypoglycemic disorder | contraindication | 237630007 | |
| Primary adrenocortical insufficiency | contraindication | 373662000 | |
| Fever | contraindication | 386661006 | |
| Surgical procedure | contraindication | 387713003 | |
| Traumatic injury | contraindication | 417746004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.79 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sulfonylurea receptor 1, Kir6.2 | Ion channel | BLOCKER | Ki | 6.46 | WOMBAT-PK | CHEMBL | |||
| Sulfonylurea receptor 2, Kir6.2 | Ion channel | BLOCKER | Ki | 4.99 | WOMBAT-PK | ||||
| Solute carrier family 22 member 6 | Transporter | Ki | 5.04 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021252 | VUID |
| N0000148693 | NUI |
| D01111 | KEGG_DRUG |
| 4021252 | VANDF |
| C0903898 | UMLSCUI |
| CHEBI:31897 | CHEBI |
| CHEMBL783 | ChEMBL_ID |
| DB00731 | DRUGBANK_ID |
| D000077715 | MESH_DESCRIPTOR_UI |
| 5311309 | PUBCHEM_CID |
| 6833 | IUPHAR_LIGAND_ID |
| 7594 | INN_ID |
| 41X3PWK4O2 | UNII |
| 274332 | RXNORM |
| 15875 | MMSL |
| 167424 | MMSL |
| d04743 | MMSL |
| 009028 | NDDF |
| 134604002 | SNOMEDCT_US |
| 387070004 | SNOMEDCT_US |
| 41X3PWK4O2 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| NATEGLINIDE | Human Prescription Drug Label | 1 | 16571-758 | TABLET | 60 mg | ORAL | ANDA | 25 sections |
| NATEGLINIDE | Human Prescription Drug Label | 1 | 16571-759 | TABLET | 120 mg | ORAL | ANDA | 25 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-656 | TABLET | 60 mg | ORAL | ANDA | 22 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-657 | TABLET | 120 mg | ORAL | ANDA | 22 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6255 | TABLET, COATED | 120 mg | ORAL | ANDA | 24 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55111-328 | TABLET | 60 mg | ORAL | ANDA | 25 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55111-329 | TABLET | 120 mg | ORAL | ANDA | 25 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-673 | TABLET | 60 mg | ORAL | ANDA | 24 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-684 | TABLET | 120 mg | ORAL | ANDA | 24 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64380-167 | TABLET | 60 mg | ORAL | ANDA | 22 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64380-168 | TABLET | 120 mg | ORAL | ANDA | 22 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68382-721 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 25 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68382-722 | TABLET, FILM COATED | 120 mg | ORAL | ANDA | 25 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1015 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 1 sections |
| Nateglinide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1016 | TABLET, FILM COATED | 120 mg | ORAL | ANDA | 1 sections |
| Nateglinide | Human Prescription Drug Label | 1 | 71209-030 | TABLET, COATED | 60 mg | ORAL | ANDA | 25 sections |
| Nateglinide | Human Prescription Drug Label | 1 | 71209-031 | TABLET, COATED | 120 mg | ORAL | ANDA | 25 sections |
| Nateglinide | Human Prescription Drug Label | 1 | 72241-002 | TABLET, COATED | 60 mg | ORAL | ANDA | 25 sections |
| Nateglinide | Human Prescription Drug Label | 1 | 72241-003 | TABLET, COATED | 120 mg | ORAL | ANDA | 25 sections |
| NATEGLINIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 75834-205 | TABLET, COATED | 60 mg | ORAL | ANDA | 28 sections |
| NATEGLINIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 75834-206 | TABLET, COATED | 120 mg | ORAL | ANDA | 28 sections |