insulin degludec Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	4960	844439-96-9

Description:

Molecule	Description
Synonyms: insulin degludec tresiba NN1250	insulin degludec is a long-acting basal human insulin analog for subcutaneous injection, differs from human insulin in that the amino acid threonine in position B30 has been omitted and a side-chain consisting of glutamic acid and a C16 fatty acid has been attached Molecular weight: 6104.04 Formula: C274H411N65O81S6 CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: 2356.52 ALOGS: ROTB: None

Molecule

Description

Synonyms:

insulin degludec
tresiba
NN1250

insulin degludec is a long-acting basal human insulin analog for subcutaneous injection, differs from human insulin in that the amino acid threonine in position B30 has been omitted and a side-chain consisting of glutamic acid and a C16 fatty acid has been attached

Molecular weight: 6104.04
Formula: C274H411N65O81S6
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA: 2356.52
ALOGS:
ROTB: None

Drug dosage:

Dose	Unit	Route
40	U	P
40	U	P
40	U	P

ADMET properties:

None

Approvals:

Date	Agency	Company
Sept. 25, 2015	FDA	NOVO NORDISK INC
Jan. 21, 2013	EMA
Sept. 28, 2012	PMDA	Novo Nordisk Pharma Ltd

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
Hypoglycaemia	746.86	17.43	290	7408	58723	53282645
Blood glucose increased	341.93	17.43	183	7515	77178	53264190
Diabetic ketoacidosis	305.58	17.43	113	7585	19802	53321566
Blood glucose decreased	156.33	17.43	70	7628	19946	53321422
Diabetes mellitus inadequate control	134.39	17.43	57	7641	14253	53327115
Blood glucose fluctuation	112.91	17.43	37	7661	4514	53336854
Diabetic neuropathy	109.10	17.43	35	7663	3992	53337376
Hyperglycaemia	91.06	17.43	62	7636	40022	53301346
Glycosylated haemoglobin increased	88.54	17.43	40	7658	11615	53329753
Hypoglycaemic coma	84.05	17.43	26	7672	2632	53338736
Hypoglycaemic unconsciousness	78.63	17.43	19	7679	759	53340609
Impaired gastric emptying	74.97	17.43	33	7665	9010	53332358
Diabetic retinopathy	57.21	17.43	19	7679	2413	53338955
Ketoacidosis	49.55	17.43	20	7678	4406	53336962
Heart sounds	48.64	17.43	12	7686	523	53340845
Retinopathy	43.22	17.43	16	7682	2796	53338572
Blood glucose abnormal	42.87	17.43	21	7677	7298	53334070
Prolonged expiration	41.82	17.43	11	7687	621	53340747
Taste disorder	38.30	17.43	20	7678	7948	53333420
Neuropathy peripheral	37.25	17.43	59	7639	103128	53238240
Hypoglycaemic encephalopathy	33.72	17.43	8	7690	295	53341073
Depressive symptom	30.61	17.43	13	7685	3251	53338117
Appetite disorder	30.24	17.43	16	7682	6527	53334841
Fear-related avoidance of activities	29.63	17.43	6	7692	104	53341264
Hypoglycaemic seizure	29.28	17.43	8	7690	522	53340846
Hypoglycaemia unawareness	29.21	17.43	6	7692	112	53341256
Acute painful neuropathy of rapid glycaemic control	29.14	17.43	4	7694	3	53341365
Sleep disorder due to a general medical condition	28.28	17.43	16	7682	7441	53333927
Diabetic metabolic decompensation	27.75	17.43	10	7688	1618	53339750
Intentional overdose	26.44	17.43	40	7658	67165	53274203
Suicide attempt	24.86	17.43	36	7662	58132	53283236
Carcinoid crisis	24.82	17.43	6	7692	240	53341128
Ketosis	24.29	17.43	7	7691	555	53340813
Respiration abnormal	24.11	17.43	13	7685	5505	53335863
Hyperkalaemia	23.80	17.43	34	7664	54222	53287146
Product prescribing error	21.06	17.43	21	7677	23010	53318358
Rales	20.50	17.43	15	7683	10817	53330551
Prerenal failure	20.43	17.43	8	7690	1626	53339742
Rheumatoid arthritis	20.34	17.43	10	7688	314521	53026847
Device failure	20.18	17.43	12	7686	6123	53335245
Presbyopia	19.90	17.43	6	7692	557	53340811
Retinal degeneration	19.46	17.43	6	7692	600	53340768
Thirst decreased	19.22	17.43	5	7693	270	53341098
Lactic acidosis	18.83	17.43	25	7673	37228	53304140
Erysipelas	18.26	17.43	12	7686	7289	53334079
Drug intolerance	17.68	17.43	4	7694	205489	53135879
Haemorrhagic disorder	17.66	17.43	6	7692	816	53340552

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	600.35	18.70	273	6807	54109	32452337
Appendicolith	249.86	18.70	69	7011	3096	32503350
Blood glucose increased	202.59	18.70	143	6937	65098	32441348
Appendicitis	179.48	18.70	69	7011	8868	32497578
Diabetic ketoacidosis	178.12	18.70	84	6996	17848	32488598
Cardiogenic shock	149.40	18.70	78	7002	20584	32485862
Blood glucose decreased	139.30	18.70	65	7015	13469	32492977
Stress	120.37	18.70	71	7009	23711	32482735
Ascites	110.60	18.70	82	6998	40109	32466337
Diabetes mellitus inadequate control	108.21	18.70	55	7025	13713	32492733
Abdominal distension	103.16	18.70	87	6993	51208	32455238
Hypoglycaemic unconsciousness	88.25	18.70	23	7057	823	32505623
Impaired gastric emptying	81.63	18.70	30	7050	3396	32503050
Multiple organ dysfunction syndrome	71.67	18.70	82	6998	69772	32436674
Glycosylated haemoglobin increased	68.75	18.70	37	7043	10352	32496094
Hyperglycaemia	60.95	18.70	57	7023	38334	32468112
General physical health deterioration	55.56	18.70	94	6986	115165	32391281
Hyponatraemia	53.24	18.70	73	7007	74440	32432006
Abdominal pain	50.87	18.70	105	6975	149424	32357022
Nausea	42.18	18.70	159	6921	320690	32185756
Constipation	39.76	18.70	86	6994	126287	32380159
Hypoglycaemic seizure	39.14	18.70	10	7070	330	32506116
Sepsis	37.89	18.70	97	6983	158737	32347709
Pancreatic carcinoma	37.33	18.70	23	7057	8283	32498163
Hypoglycaemia unawareness	36.43	18.70	8	7072	135	32506311
Ventricular fibrillation	33.99	18.70	29	7051	17281	32489165
Vomiting	33.62	18.70	120	6960	235437	32271009
Hypoglycaemic coma	32.33	18.70	14	7066	2429	32504017
Hyperkinetic heart syndrome	31.50	18.70	7	7073	125	32506321
Suicide attempt	31.17	18.70	40	7040	38204	32468242
Toxicity to various agents	28.18	18.70	3	7077	178038	32328408
Pancreatitis	28.15	18.70	38	7042	38113	32468333
Diabetic metabolic decompensation	27.59	18.70	11	7069	1551	32504895
Neuropathy peripheral	27.22	18.70	55	7025	76927	32429519
Oedematous pancreatitis	26.78	18.70	8	7072	474	32505972
Euglycaemic diabetic ketoacidosis	24.38	18.70	12	7068	2786	32503660
Ketoacidosis	22.53	18.70	13	7067	4151	32502295
Hypoglycaemic encephalopathy	21.11	18.70	6	7074	298	32506148
Diabetic foot	20.98	18.70	11	7069	2915	32503531
Blood glucose fluctuation	20.33	18.70	12	7068	3997	32502449
Blood glucose abnormal	19.02	18.70	13	7067	5575	32500871
Acute coronary syndrome	18.90	18.70	19	7061	13922	32492524

Pharmacologic Action:

Source	Code	Description
ATC	A10AD06	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES INSULINS AND ANALOGUES Insulins and analogues for injection, intermediate- or long-acting combined with fast-acting
ATC	A10AE06	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES INSULINS AND ANALOGUES Insulins and analogues for injection, long-acting
ATC	A10AE56	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES INSULINS AND ANALOGUES Insulins and analogues for injection, long-acting
FDA CS	M0011417	Insulin
FDA EPC	N0000175453	Insulin Analog
CHEBI has role	CHEBI:35526	hypoglycemic drug
FDA EPC	N0000175944	Insulin

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Diabetes mellitus	indication	73211009	DOID:9351

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Insulin receptor	Kinase	P06213	INSR_HUMAN	AGONIST				DRUG LABEL	DRUG LABEL

External reference:

ID	Source
D09727	KEGG_DRUG
4017559	VANDF
4017569	VANDF
4019786	VANDF
4035011	VANDF
CHEBI:5931	CHEBI
CHEMBL2107869	ChEMBL_ID
C571886	MESH_SUPPLEMENTAL_RECORD_UI
9170	INN_ID
5186	INN_ID
DB09564	DRUGBANK_ID
54Q18076QB	UNII
118984462	PUBCHEM_CID
118984375	PUBCHEM_CID
DB00030	DRUGBANK_ID
1670007	RXNORM
236826	MMSL
29260	MMSL
4885	MMSL
4886	MMSL
d00262	MMSL
d04369	MMSL
d08054	MMSL
000869	NDDF
000870	NDDF
006518	NDDF
015340	NDDF
126210001	SNOMEDCT_US
417423002	SNOMEDCT_US
420609005	SNOMEDCT_US
710281005	SNOMEDCT_US
715774000	SNOMEDCT_US
96367001	SNOMEDCT_US
C3491971	UMLSCUI
C0795635	UMLSCUI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Tresiba	HUMAN PRESCRIPTION DRUG LABEL	1	0169-2550	INJECTION, SOLUTION	200 U	SUBCUTANEOUS	BLA	27 sections
Tresiba	HUMAN PRESCRIPTION DRUG LABEL	1	0169-2660	INJECTION, SOLUTION	100 U	SUBCUTANEOUS	BLA	27 sections
Tresiba	HUMAN PRESCRIPTION DRUG LABEL	1	0169-2662	INJECTION, SOLUTION	100 U	SUBCUTANEOUS	BLA	27 sections
Xultophy 100/3.6	HUMAN PRESCRIPTION DRUG LABEL	2	0169-2911	INJECTION, SOLUTION	100 [iU]	SUBCUTANEOUS	BLA	27 sections
Tresiba	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3491	INJECTION, SOLUTION	200 U	SUBCUTANEOUS	BLA	28 sections