insulin degludec 🐶 Veterinary Use | 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
Jan. 21, 2013	EMA
Sept. 25, 2015	FDA	NOVO NORDISK INC
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	784.10	17.09	304	9069	59761	63419888
Diabetic ketoacidosis	374.03	17.09	133	9240	20372	63459277
Blood glucose increased	343.17	17.09	190	9183	83566	63396083
Blood glucose decreased	186.90	17.09	81	9292	20871	63458778
Diabetes mellitus inadequate control	123.60	17.09	55	9318	15071	63464578
Blood glucose fluctuation	115.88	17.09	38	9335	4538	63475111
Diabetic neuropathy	112.95	17.09	36	9337	3928	63475721
Hyperglycaemia	106.29	17.09	70	9303	41797	63437852
Heart sounds	93.38	17.09	23	9350	973	63478676
Prolonged expiration	91.20	17.09	23	9350	1073	63478576
Sleep disorder due to a general medical condition	89.05	17.09	41	9332	12147	63467502
Hypoglycaemic coma	88.52	17.09	27	9346	2548	63477101
Glycosylated haemoglobin increased	82.21	17.09	39	9334	12359	63467290
Impaired gastric emptying	70.03	17.09	33	9340	10299	63469350
Hypoglycaemic unconsciousness	68.11	17.09	17	9356	760	63478889
Depressive symptom	64.95	17.09	24	9349	4078	63475571
Appetite disorder	57.80	17.09	26	9347	7295	63472354
Diabetic retinopathy	57.61	17.09	19	9354	2308	63477341
Blood glucose abnormal	55.94	17.09	26	9347	7866	63471783
Respiration abnormal	54.55	17.09	24	9349	6393	63473256
Rales	44.28	17.09	26	9347	12671	63466978
Ketoacidosis	42.55	17.09	18	9355	4360	63475289
Joint abscess	41.09	17.09	10	9363	402	63479247
Neuropathy peripheral	35.92	17.09	62	9311	113605	63366044
Hypoglycaemia unawareness	34.76	17.09	7	9366	115	63479534
Diabetes mellitus	34.71	17.09	42	9331	55768	63423881
Stress	34.57	17.09	46	9327	67121	63412528
Intentional overdose	33.97	17.09	48	9325	74104	63405545
Fear-related avoidance of activities	33.95	17.09	7	9366	130	63479519
Hypoglycaemic encephalopathy	33.31	17.09	8	9365	304	63479345
Suicide attempt	31.78	17.09	42	9331	60876	63418773
Flank pain	31.21	17.09	23	9350	16387	63463262
Device failure	31.17	17.09	16	9357	5995	63473654
Retinopathy	30.90	17.09	13	9360	3106	63476543
Angina pectoris	29.89	17.09	29	9344	30049	63449600
Hypoglycaemic seizure	29.69	17.09	8	9365	484	63479165
Carcinoid crisis	29.32	17.09	7	9366	259	63479390
Acute painful neuropathy of rapid glycaemic control	29.05	17.09	4	9369	3	63479646
Ketosis	27.95	17.09	8	9365	605	63479044
Taste disorder	27.92	17.09	20	9353	13642	63466007
Drug intolerance	27.49	17.09	6	9367	308655	63170994
Wheezing	27.43	17.09	50	9323	95545	63384104
Toxicity to various agents	26.07	17.09	3	9370	247247	63232402
Infusion related reaction	25.83	17.09	3	9370	245518	63234131
Asthma	23.93	17.09	56	9317	127505	63352144
Thirst decreased	23.83	17.09	6	9367	278	63479371
Hospitalisation	23.77	17.09	44	9329	85037	63394612
Diabetic metabolic decompensation	23.42	17.09	9	9364	1701	63477948
Muscle necrosis	22.94	17.09	7	9366	661	63478988
Arthropathy	22.08	17.09	4	9369	234788	63244861
Retinal degeneration	20.97	17.09	7	9366	882	63478767
Presbyopia	20.82	17.09	6	9367	465	63479184
Metabolic acidosis	20.37	17.09	29	9344	45040	63434609
Hypoglycaemia neonatal	20.34	17.09	7	9366	968	63478681
Product prescribing error	20.07	17.09	22	9351	26267	63453382
Depressed mood	19.87	17.09	27	9346	40164	63439485
Infective myositis	19.85	17.09	4	9369	66	63479583
Contraindicated product administered	19.84	17.09	4	9369	217644	63262005
Reperfusion arrhythmia	19.70	17.09	5	9368	239	63479410
Dyspnoea exertional	19.17	17.09	33	9340	60269	63419380
Nasal congestion	18.39	17.09	34	9339	65626	63414023
Intestinal ulcer	17.81	17.09	7	9366	1404	63478245
Drug ineffective	17.67	17.09	87	9286	1044678	62434971
Loss of personal independence in daily activities	17.47	17.09	42	9331	97248	63382401
Treatment failure	17.44	17.09	4	9369	199039	63280610
Haemorrhagic disorder	17.29	17.09	6	9367	850	63478799
Erysipelas	17.14	17.09	12	9361	7893	63471756

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	475.22	20.47	253	9527	54387	34892764
Appendicolith	452.75	20.47	145	9635	8456	34938695
Appendicitis	375.70	20.47	145	9635	14662	34932489
Cardiogenic shock	327.14	20.47	156	9624	26462	34920689
Stress	287.39	20.47	149	9631	30198	34916953
Ascites	252.90	20.47	159	9621	46412	34900739
Abdominal distension	215.38	20.47	157	9623	58335	34888816
Ventricular fibrillation	203.77	20.47	108	9672	22846	34924305
Blood glucose increased	188.47	20.47	153	9627	66565	34880586
Blood phosphorus increased	182.88	20.47	72	9708	7649	34939502
Multiple organ dysfunction syndrome	170.12	20.47	153	9627	76413	34870738
Diabetic ketoacidosis	160.44	20.47	85	9695	17947	34929204
Hyponatraemia	156.24	20.47	151	9629	82540	34864611
General physical health deterioration	140.76	20.47	176	9604	128093	34819058
Blood glucose decreased	133.81	20.47	68	9712	13169	34933982
Constipation	116.51	20.47	166	9614	136816	34810335
Dry mouth	106.38	20.47	79	9701	30086	34917065
Abdominal pain	106.32	20.47	175	9605	163443	34783708
Sepsis	105.35	20.47	176	9604	166385	34780766
Diabetes mellitus inadequate control	91.03	20.47	53	9727	13411	34933740
Vomiting	87.63	20.47	205	9575	247416	34699735
Hypoglycaemic unconsciousness	83.85	20.47	23	9757	775	34946376
Nausea	79.31	20.47	241	9539	339667	34607484
Myasthenia gravis	77.02	20.47	38	9742	6902	34940249
Impaired gastric emptying	74.08	20.47	30	9750	3423	34943728
Blood uric acid increased	70.70	20.47	40	9740	9584	34937567
Glycosylated haemoglobin increased	45.12	20.47	32	9748	11328	34935823
Somnolence	44.69	20.47	97	9683	111019	34836132
Hyperglycaemia	44.44	20.47	55	9725	39425	34907726
Blood cholesterol increased	43.41	20.47	40	9740	20503	34926648
Drug therapy	43.08	20.47	15	9765	1126	34946025
Incorrect route of product administration	41.68	20.47	34	9746	14811	34932340
Analgesic therapy	41.10	20.47	14	9766	984	34946167
Sleep disorder therapy	36.90	20.47	13	9767	1010	34946141
Hyperphosphataemia	36.85	20.47	20	9760	4417	34942734
Hypoglycaemic seizure	36.80	20.47	10	9770	325	34946826
Hypoglycaemia unawareness	34.21	20.47	8	9772	139	34947012
Hypoglycaemic coma	32.09	20.47	15	9765	2416	34944735
Iron deficiency	30.69	20.47	19	9761	5362	34941789
Blood glucose fluctuation	27.53	20.47	16	9764	4028	34943123
Dysmetria	26.83	20.47	9	9771	603	34946548
Bacterial infection	26.34	20.47	28	9752	17035	34930116
Oedematous pancreatitis	24.56	20.47	8	9772	489	34946662
Neuralgia	23.68	20.47	25	9755	15088	34932063
Diabetic metabolic decompensation	23.63	20.47	11	9769	1755	34945396
Condition aggravated	23.39	20.47	111	9669	192085	34755066
Euglycaemic diabetic ketoacidosis	22.60	20.47	13	9767	3209	34943942
Gait spastic	21.73	20.47	9	9771	1087	34946064
Neuropathy peripheral	21.09	20.47	61	9719	83202	34863949

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
Hypoglycaemia	936.75	15.94	448	16532	101146	79626262
Appendicolith	487.78	15.94	144	16836	8407	79719001
Diabetic ketoacidosis	431.85	15.94	188	16792	33934	79693474
Appendicitis	365.90	15.94	145	16835	20649	79706759
Blood glucose increased	354.54	15.94	249	16731	114726	79612682
Cardiogenic shock	299.88	15.94	156	16824	41758	79685650
Stress	291.87	15.94	192	16788	79420	79647988
Ascites	226.53	15.94	161	16819	75401	79652007
Ventricular fibrillation	197.77	15.94	108	16872	31818	79695590
Abdominal distension	186.43	15.94	174	16806	119476	79607932
Diabetes mellitus inadequate control	184.10	15.94	94	16886	24170	79703238
Blood phosphorus increased	181.39	15.94	72	16908	10275	79717133
Blood glucose decreased	154.91	15.94	86	16894	26148	79701260
Multiple organ dysfunction syndrome	148.40	15.94	154	16826	120092	79607316
Impaired gastric emptying	140.53	15.94	60	16920	10293	79717115
Hyperglycaemia	124.58	15.94	110	16870	70225	79657183
Diabetic neuropathy	118.60	15.94	46	16934	6170	79721238
Hypoglycaemic unconsciousness	118.47	15.94	31	16949	1152	79726256
Hyponatraemia	116.20	15.94	165	16815	177683	79549725
Blood glucose fluctuation	111.91	15.94	45	16935	6637	79720771
Hypoglycaemic coma	104.41	15.94	39	16941	4721	79722687
Sepsis	95.42	15.94	190	16790	269238	79458170
Constipation	92.42	15.94	193	16787	282857	79444551
General physical health deterioration	90.24	15.94	188	16792	275050	79452358
Glycosylated haemoglobin increased	86.80	15.94	53	16927	19207	79708201
Heart sounds	85.71	15.94	23	16957	943	79726465
Prolonged expiration	79.46	15.94	23	16957	1248	79726160
Dry mouth	73.28	15.94	92	16888	87927	79639481
Myasthenia gravis	72.27	15.94	38	16942	10361	79717047
Sleep disorder due to a general medical condition	71.37	15.94	42	16938	14235	79713173
Toxicity to various agents	70.53	15.94	5	16975	421535	79305873
Blood uric acid increased	68.62	15.94	40	16940	13320	79714088
Abdominal pain	65.70	15.94	207	16773	389362	79338046
Hypoglycaemia unawareness	64.76	15.94	14	16966	224	79727184
Neuropathy peripheral	62.88	15.94	110	16870	141195	79586213
Ketoacidosis	55.43	15.94	29	16951	7825	79719583
Hypoglycaemic seizure	51.91	15.94	15	16965	809	79726599
Hypoglycaemic encephalopathy	50.54	15.94	14	16966	647	79726761
Appetite disorder	50.17	15.94	27	16953	7712	79719696
Diabetic retinopathy	48.86	15.94	20	16960	3086	79724322
Diabetic metabolic decompensation	47.50	15.94	20	16960	3312	79724096
Drug therapy	46.34	15.94	15	16965	1186	79726222
Vomiting	46.19	15.94	270	16710	665558	79061850
Nausea	45.37	15.94	353	16627	956843	78770565
Analgesic therapy	44.70	15.94	14	16966	995	79726413
Depressive symptom	43.30	15.94	23	16957	6400	79721008
Blood glucose abnormal	42.36	15.94	27	16953	10539	79716869
Respiration abnormal	41.81	15.94	24	16956	7764	79719644
Sleep disorder therapy	40.37	15.94	13	16967	1011	79726397
Hyperphosphataemia	37.88	15.94	21	16959	6355	79721053
Euglycaemic diabetic ketoacidosis	36.50	15.94	21	16959	6823	79720585
Joint abscess	34.74	15.94	10	16970	532	79726876
Fear-related avoidance of activities	32.99	15.94	7	16973	102	79727306
Rales	32.85	15.94	30	16950	19971	79707437
Suicide attempt	31.10	15.94	60	16920	82872	79644536
Drug ineffective	29.18	15.94	125	16855	1080788	78646620
Incorrect route of product administration	28.23	15.94	36	16944	34893	79692515
Acute painful neuropathy of rapid glycaemic control	27.58	15.94	4	16976	3	79727405
Intentional overdose	27.46	15.94	66	16914	105894	79621514
Somnolence	27.35	15.94	112	16868	238869	79488539
Oedematous pancreatitis	27.19	15.94	10	16970	1158	79726250
Arthropathy	27.15	15.94	3	16977	177108	79550300
Infusion related reaction	26.57	15.94	8	16972	230229	79497179
Iron deficiency	25.81	15.94	20	16960	10634	79716774
Therapeutic product effect decreased	24.56	15.94	3	16977	163860	79563548
Drug abuse	24.33	15.94	3	16977	162688	79564720
Joint swelling	23.99	15.94	16	16964	288630	79438778
Retinopathy	23.62	15.94	13	16967	3878	79723530
Pancreatic carcinoma	23.54	15.94	21	16959	13556	79713852
Treatment failure	23.51	15.94	4	16976	170482	79556926
Diabetic foot infection	22.90	15.94	8	16972	799	79726609
Carcinoid crisis	22.10	15.94	7	16973	516	79726892
Flank pain	21.92	15.94	24	16956	19820	79707588
Diabetic foot	21.68	15.94	12	16968	3620	79723788
Thirst decreased	21.07	15.94	6	16974	307	79727101
Tachycardia	20.83	15.94	6	16974	177762	79549646
Incorrect dose administered by device	20.63	15.94	13	16967	4976	79722432
Synovitis	19.79	15.94	4	16976	150730	79576678
Taste disorder	19.00	15.94	20	16960	15803	79711605
Sinusitis	18.88	15.94	9	16971	195492	79531916
Disease progression	18.56	15.94	8	16972	184354	79543054
Neutropenia	17.83	15.94	21	16959	287689	79439719
Bacterial infection	17.46	15.94	27	16953	31253	79696155
Arthralgia	17.35	15.94	63	16917	571740	79155668
Presbyopia	17.25	15.94	6	16974	592	79726816
Cerebral infarction	17.06	15.94	33	16947	45643	79681765
Reperfusion arrhythmia	16.87	15.94	5	16975	295	79727113
Ketosis	16.86	15.94	7	16973	1119	79726289
Thrombocytopenia	16.82	15.94	19	16961	265240	79462168
Hypotension	16.54	15.94	44	16936	440273	79287135
Urogenital infection fungal	16.39	15.94	3	16977	19	79727389
Diabetes mellitus	16.34	15.94	45	16935	78345	79649063

FDA Adverse Event Reporting System (Pediatric)

None

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	antidiabetic
FDA EPC	N0000175944	Insulin

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

Disease	Relation	SNOMED_ID	DOID
Diabetes mellitus	indication	73211009	DOID:9351

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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
DB09564	DRUGBANK_ID
DB00030	DRUGBANK_ID
1670007	RXNORM
236826	MMSL
29260	MMSL
361472	MMSL
366445	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
9170	INN_ID
118984462	PUBCHEM_CID
5186	INN_ID
118984375	PUBCHEM_CID
54Q18076QB	UNII

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	28 sections
Tresiba	HUMAN PRESCRIPTION DRUG LABEL	1	0169-2550	INJECTION, SOLUTION	200 U	SUBCUTANEOUS	BLA	28 sections
Tresiba	HUMAN PRESCRIPTION DRUG LABEL	1	0169-2660	INJECTION, SOLUTION	100 U	SUBCUTANEOUS	BLA	28 sections
Tresiba	HUMAN PRESCRIPTION DRUG LABEL	1	0169-2660	INJECTION, SOLUTION	100 U	SUBCUTANEOUS	BLA	28 sections
Tresiba	HUMAN PRESCRIPTION DRUG LABEL	1	0169-2662	INJECTION, SOLUTION	100 U	SUBCUTANEOUS	BLA	28 sections
Tresiba	HUMAN PRESCRIPTION DRUG LABEL	1	0169-2662	INJECTION, SOLUTION	100 U	SUBCUTANEOUS	BLA	28 sections
Xultophy 100/3.6	HUMAN PRESCRIPTION DRUG LABEL	2	0169-2911	INJECTION, SOLUTION	100 [iU]	SUBCUTANEOUS	BLA	27 sections
Xultophy 100/3.6	HUMAN PRESCRIPTION DRUG LABEL	2	0169-2911	INJECTION, SOLUTION	100 [iU]	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
Tresiba	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3491	INJECTION, SOLUTION	200 U	SUBCUTANEOUS	BLA	28 sections
Insulin Degludec	HUMAN PRESCRIPTION DRUG LABEL	1	73070-400	INJECTION, SOLUTION	100 U	SUBCUTANEOUS	BLA	27 sections
Insulin Degludec	HUMAN PRESCRIPTION DRUG LABEL	1	73070-403	INJECTION, SOLUTION	100 U	SUBCUTANEOUS	BLA	27 sections
Insulin Degludec	HUMAN PRESCRIPTION DRUG LABEL	1	73070-503	INJECTION, SOLUTION	200 U	SUBCUTANEOUS	BLA	27 sections