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

Stem definition	Drug id	CAS RN
antihyperglycaemics	2366	135062-02-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: repaglinide (S)-(+)-Repaglinide prandin enyglid surepost	Molecular weight: 452.60 Formula: C27H36N2O4 CLOGP: 5.66 LIPINSKI: 1 HAC: 6 HDO: 2 TPSA: 78.87 ALOGS: -5.19 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

repaglinide
(S)-(+)-Repaglinide
prandin
enyglid
surepost

Molecular weight: 452.60
Formula: C27H36N2O4
CLOGP: 5.66
LIPINSKI: 1
HAC: 6
HDO: 2
TPSA: 78.87
ALOGS: -5.19
ROTB: 10

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
4	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	7.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	56 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	1.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.47 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
t_half (Half-life)	0.87 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.35 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.04 mg/mL	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 22, 1997	FDA	NOVO NORDISK INC

FDA Adverse Event Reporting System (Female)

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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	665.61	17.19	270	9077	59795	63419880
Lactic acidosis	365.53	17.19	155	9192	38132	63441543
Acute kidney injury	319.47	17.19	282	9065	263133	63216542
Hypoglycaemic coma	180.04	17.19	47	9300	2528	63477147
Drug interaction	120.54	17.19	158	9189	228973	63250702
Hyperkalaemia	119.66	17.19	83	9264	54120	63425555
Diabetes mellitus inadequate control	80.74	17.19	41	9306	15085	63464590
Pemphigoid	77.54	17.19	32	9315	7312	63472363
Blood glucose increased	69.35	17.19	73	9274	83683	63395992
Sopor	66.11	17.19	41	9306	22123	63457552

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FDA Adverse Event Reporting System (Male)

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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	689.28	15.46	340	10911	54300	34891380
Lactic acidosis	283.14	15.46	162	11089	34610	34911070
Hypoglycaemic coma	175.56	15.46	54	11197	2377	34943303
Acute kidney injury	167.02	15.46	327	10924	304661	34641019
Drug interaction	111.01	15.46	232	11019	225714	34719966
Pemphigoid	56.37	15.46	35	11216	8631	34937049
Diabetes mellitus inadequate control	53.29	15.46	40	11211	13424	34932256
Hyperkalaemia	52.47	15.46	86	11165	69303	34876377
Sopor	50.15	15.46	37	11214	12099	34933581
Oesophageal perforation	47.75	15.46	17	11234	1182	34944498

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FDA Adverse Event Reporting System (Geriatric)

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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	1247.02	14.18	569	18868	101025	79623926
Lactic acidosis	621.29	14.18	315	19122	70044	79654907
Acute kidney injury	444.03	14.18	586	18851	518818	79206133
Hypoglycaemic coma	365.00	14.18	104	19333	4656	79720295
Drug interaction	228.68	14.18	382	19055	414801	79310150
Hyperkalaemia	154.94	14.18	164	19273	114234	79610717
Pemphigoid	133.20	14.18	68	19369	15247	79709704
Diabetes mellitus inadequate control	104.08	14.18	68	19369	24196	79700755
Sopor	102.83	14.18	76	19361	32934	79692017
Hyperglycaemia	91.91	14.18	99	19338	70236	79654715

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A10BD14	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BX02	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

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

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Disease	Relation	SNOMED_ID	DOID
Diabetes mellitus type 2	indication	44054006	DOID:9352
Alcoholism	contraindication	7200002
Asthenia	contraindication	13791008
Myocardial infarction	contraindication	22298006	DOID:5844
Acute vomiting	contraindication	23971007
Severe adrenal insufficiency	contraindication	24867002
Alcohol intoxication	contraindication	25702006
Shock	contraindication	27942005
Dehydration	contraindication	34095006
Infectious disease	contraindication	40733004

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.43	acidic
pKa2	3.8	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sulfonylurea receptor 1, Kir6.2	Ion channel	Q09428 Q14654	ABCC8_HUMAN KCJ11_HUMAN	BLOCKER	Ki	9.14	WOMBAT-PK	CHEMBL
ATP-binding cassette sub-family C member 8	Ion channel	Q09428	ABCC8_HUMAN		Kd	7.30	CHEMBL
Solute carrier organic anion transporter family member 1B1	Transporter	Q9Y6L6	SO1B1_HUMAN				WOMBAT-PK
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	5.04	CHEMBL
Sulfonylurea receptor 2, Kir6.2	Ion channel	O60706 Q14654	ABCC9_HUMAN KCJ11_HUMAN	BLOCKER	Ki	8.81	WOMBAT-PK

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External reference:

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ID	Source
BJX	PDB_CHEM_ID
007421	NDDF
109074004	SNOMEDCT_US
11576	MMSL
120643	MMSL
219335	RXNORM
386964000	SNOMEDCT_US
4021119	VUID
4021119	VANDF
5416	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Prandin	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5381	TABLET	2 mg	ORAL	NDA	21 sections
Prandin	HUMAN PRESCRIPTION DRUG LABEL	1	54868-6439	TABLET	1 mg	ORAL	NDA	21 sections
Prandin	HUMAN PRESCRIPTION DRUG LABEL	1	60846-882	TABLET	1 mg	ORAL	ANDA	28 sections
Prandin	HUMAN PRESCRIPTION DRUG LABEL	1	60846-884	TABLET	2 mg	ORAL	ANDA	28 sections
Repaglinide	HUMAN PRESCRIPTION DRUG LABEL	1	0574-0240	TABLET	0.50 mg	ORAL	ANDA	25 sections
Repaglinide	HUMAN PRESCRIPTION DRUG LABEL	1	0574-0240	TABLET	0.50 mg	ORAL	ANDA	25 sections
Repaglinide	HUMAN PRESCRIPTION DRUG LABEL	1	0574-0241	TABLET	1 mg	ORAL	ANDA	25 sections
Repaglinide	HUMAN PRESCRIPTION DRUG LABEL	1	0574-0241	TABLET	1 mg	ORAL	ANDA	25 sections
Repaglinide	HUMAN PRESCRIPTION DRUG LABEL	1	0574-0242	TABLET	2 mg	ORAL	ANDA	25 sections
Repaglinide	HUMAN PRESCRIPTION DRUG LABEL	1	0574-0242	TABLET	2 mg	ORAL	ANDA	25 sections

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