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

Stem definition	Drug id	CAS RN
analgesics	4283	175591-09-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: tapentadol tapentadol hydrochloride nucynta tapentadol HCl	An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES. Molecular weight: 221.34 Formula: C14H23NO CLOGP: 3.15 LIPINSKI: 0 HAC: 2 HDO: 1 TPSA: 23.47 ALOGS: -2.45 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tapentadol
tapentadol hydrochloride
nucynta
tapentadol HCl

An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES.

Molecular weight: 221.34
Formula: C14H23NO
CLOGP: 3.15
LIPINSKI: 0
HAC: 2
HDO: 1
TPSA: 23.47
ALOGS: -2.45
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.40	g	O

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	4.64 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	21.33 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.39 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	1.16 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
Nov. 20, 2008	FDA	JANSSEN PHARMS

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
Drug interaction	130.26	15.29	183	11369	228948	63248522
Sopor	108.88	15.29	61	11491	22103	63455367
Serotonin syndrome	101.79	15.29	64	11488	28618	63448852
Toxicity to various agents	101.67	15.29	170	11382	247080	63230390
Paroxysmal extreme pain disorder	72.46	15.29	13	11539	87	63477383
Degenerative bone disease	71.25	15.29	14	11538	161	63477309
Chronic respiratory disease	70.10	15.29	14	11538	176	63477294
Confusional arousal	68.70	15.29	14	11538	196	63477274
Drug abuse	66.95	15.29	74	11478	72444	63405026
Post procedural hypothyroidism	64.73	15.29	14	11538	265	63477205
Agitation	60.44	15.29	64	11488	59693	63417777
Confusional state	59.38	15.29	132	11420	236248	63241222
HIV infection	58.93	15.29	14	11538	409	63477061
Somnolence	54.42	15.29	108	11444	178577	63298893
Overdose	49.68	15.29	81	11471	114997	63362473
Respiratory depression	49.64	15.29	31	11521	13684	63463786
Delirium	47.36	15.29	52	11500	50489	63426981
Mouth injury	46.76	15.29	14	11538	1003	63476467
Restlessness	45.82	15.29	40	11512	29413	63448057
Intentional overdose	43.12	15.29	60	11492	74092	63403378
Reflexes abnormal	43.01	15.29	12	11540	669	63476801
Polymyalgia rheumatica	41.41	15.29	18	11534	3773	63473697
Miosis	40.96	15.29	22	11530	7331	63470139
Suicide attempt	38.00	15.29	51	11501	60867	63416603
Sepsis neonatal	37.58	15.29	10	11542	466	63477004
Completed suicide	37.25	15.29	82	11470	145591	63331879
Hypertensive crisis	37.18	15.29	27	11525	15259	63462211
Eyelid skin dryness	36.38	15.29	8	11544	164	63477306
Unresponsive to stimuli	35.57	15.29	37	11515	33779	63443691
Tongue discomfort	35.55	15.29	14	11538	2289	63475181
Embolism venous	34.53	15.29	15	11537	3139	63474331
Loss of consciousness	34.25	15.29	70	11482	118051	63359419
Suicidal ideation	34.05	15.29	49	11503	62372	63415098
Abdominal discomfort	32.66	15.29	9	11543	320876	63156594
Disorientation	32.55	15.29	38	11514	39414	63438056
Accidental exposure to product by child	32.40	15.29	11	11541	1182	63476288
Abnormal dreams	31.24	15.29	21	11531	10495	63466975
Amnestic disorder	31.22	15.29	8	11544	321	63477149
Mydriasis	31.10	15.29	22	11530	11934	63465536
Tremor	31.08	15.29	72	11480	132167	63345303
Chemical burn of oral cavity	30.69	15.29	6	11546	67	63477403
Renal cell carcinoma stage I	30.02	15.29	5	11547	20	63477450
Hallucination	29.85	15.29	43	11509	54774	63422696
Application site injury	28.94	15.29	5	11547	26	63477444
Seizure	28.77	15.29	70	11482	132564	63344906
Depressed level of consciousness	28.55	15.29	45	11507	62033	63415437
Allodynia	28.06	15.29	9	11543	810	63476660
Systemic lupus erythematosus	27.45	15.29	3	11549	208915	63268555
Drug screen negative	27.13	15.29	7	11545	289	63477181
Drug withdrawal syndrome neonatal	26.44	15.29	11	11541	2070	63475400
Peptic ulcer	26.32	15.29	14	11538	4573	63472897
Malignant neoplasm progression	25.39	15.29	50	11502	82071	63395399
Clubbing	24.29	15.29	7	11545	439	63477031
Tender joint count	23.81	15.29	6	11546	225	63477245
Hyperhidrosis	23.47	15.29	57	11495	107779	63369691
Middle insomnia	23.43	15.29	19	11533	12624	63464846
Gaze palsy	23.22	15.29	9	11543	1411	63476059
Application site ulcer	22.86	15.29	5	11547	100	63477370
Opiates negative	22.84	15.29	3	11549	0	63477470
Nasal polyps	22.73	15.29	14	11538	6025	63471445
Concomitant disease aggravated	21.94	15.29	16	11536	9096	63468374
Osteopenia	21.44	15.29	22	11530	19763	63457707
Urinary retention	21.43	15.29	27	11525	30274	63447196
Product prescribing error	21.14	15.29	25	11527	26264	63451206
Maternal exposure during pregnancy	20.88	15.29	7	11545	220055	63257415
Bradyphrenia	20.88	15.29	14	11538	6966	63470504
Bundle branch block left	20.73	15.29	14	11538	7045	63470425
Myoclonic epilepsy	20.69	15.29	8	11544	1246	63476224
Drug screen positive	20.61	15.29	11	11541	3618	63473852
Lymphoedema	20.47	15.29	17	11535	11675	63465795
Labelled drug-drug interaction medication error	20.43	15.29	18	11534	13381	63464089
Dyslipidaemia	20.15	15.29	14	11538	7379	63470091
Synovectomy	19.91	15.29	5	11547	185	63477285
Wound	19.86	15.29	3	11549	163260	63314210
Infusion related reaction	19.76	15.29	10	11542	245511	63231959
Arthropathy	19.75	15.29	9	11543	234783	63242687
Pharyngeal enanthema	19.69	15.29	4	11548	55	63477415
Joint swelling	18.96	15.29	19	11533	327647	63149823
Constipation	18.87	15.29	86	11466	224857	63252613
Hyperresponsive to stimuli	18.74	15.29	4	11548	71	63477399
Aortic valve stenosis	18.73	15.29	10	11542	3289	63474181
Gingivitis	18.50	15.29	14	11538	8415	63469055
Bacteriuria	18.38	15.29	7	11545	1046	63476424
Logorrhoea	18.29	15.29	9	11543	2501	63474969
Thoracic vertebral fracture	18.19	15.29	11	11541	4581	63472889
Withdrawal syndrome	17.73	15.29	20	11532	19977	63457493
Sedation	17.65	15.29	28	11524	38781	63438689
Tachycardia	17.28	15.29	54	11498	118102	63359368
Dyskinesia	17.27	15.29	25	11527	31977	63445493
Synovial disorder	16.92	15.29	8	11544	2037	63475433
Aggression	16.71	15.29	21	11531	23477	63453993
Disturbance in attention	16.61	15.29	27	11525	38162	63439308
Stenosis	16.20	15.29	7	11545	1447	63476023
Total bile acids increased	16.17	15.29	4	11548	139	63477331
Radiculopathy	16.08	15.29	13	11539	8598	63468872
Drug screen false positive	15.88	15.29	6	11546	878	63476592
Lumbar vertebral fracture	15.83	15.29	11	11541	5799	63471671

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
Serotonin syndrome	116.81	18.80	62	6418	19871	34930580
Delirium	106.67	18.80	78	6402	43913	34906538
Quality of life decreased	85.53	18.80	31	6449	3970	34946481
Hyperaesthesia	77.55	18.80	30	6450	4600	34945851
Drug abuse	75.01	18.80	92	6388	99004	34851447
Constipation	72.82	18.80	107	6373	136875	34813576
Suicide attempt	61.84	18.80	54	6426	39062	34911389
Toxicity to various agents	60.80	18.80	122	6358	200240	34750211
Sopor	55.28	18.80	32	6448	12104	34938347
Overdose	54.00	18.80	75	6405	90984	34859467
Polyneuropathy in malignant disease	49.44	18.80	11	6469	234	34950217
Allodynia	49.30	18.80	14	6466	817	34949634
Confusional state	43.89	18.80	88	6392	144072	34806379
Intentional overdose	42.12	18.80	46	6434	43628	34906823
Drug dependence	39.40	18.80	34	6446	24183	34926268
Withdrawal syndrome	36.90	18.80	25	6455	12430	34938021
Somnolence	32.79	18.80	67	6413	111049	34839402
Application site hypersensitivity	32.57	18.80	7	6473	126	34950325
Hallucination	31.35	18.80	43	6437	51455	34898996
Respiratory depression	30.96	18.80	25	6455	16220	34934231
Drug interaction	30.95	18.80	102	6378	225844	34724607
Malignant neoplasm progression	30.73	18.80	57	6423	87989	34862462
Adverse event	29.68	18.80	26	6454	18851	34931600
Xanthelasma	28.64	18.80	6	6474	95	34950356
Drug screen positive	25.16	18.80	13	6467	3930	34946521
Accidental exposure to product by child	22.72	18.80	9	6471	1467	34948984
Post herpetic neuralgia	21.97	18.80	8	6472	1037	34949414
Myofascial pain syndrome	20.79	18.80	6	6474	371	34950080
Product prescribing error	20.11	18.80	23	6457	22904	34927547
Tremor	19.99	18.80	46	6434	82541	34867910
Loss of consciousness	19.96	18.80	46	6434	82621	34867830
Tobacco abuse	19.79	18.80	6	6474	440	34950011
Oromandibular dystonia	19.11	18.80	6	6474	495	34949956

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
Toxicity to various agents	154.81	15.54	279	14561	421261	79308287
Sopor	149.97	15.54	87	14753	32923	79696625
Serotonin syndrome	129.90	15.54	89	14751	44938	79684610
Delirium	129.72	15.54	115	14725	84512	79645036
Drug abuse	128.93	15.54	155	14685	162536	79567012
Drug interaction	125.42	15.54	253	14587	414930	79314618
Confusional state	87.89	15.54	187	14653	317810	79411738
Suicide attempt	84.32	15.54	90	14750	82842	79646706
Intentional overdose	79.06	15.54	98	14742	105862	79623686
Respiratory depression	78.21	15.54	54	14786	27576	79701972
Allodynia	76.63	15.54	23	14817	1625	79727923
Accidental exposure to product by child	75.08	15.54	26	14814	2900	79726648
Overdose	73.89	15.54	127	14713	184079	79545469
Somnolence	72.38	15.54	146	14694	238835	79490713
Hyperaesthesia	71.32	15.54	38	14802	12184	79717364
Constipation	62.09	15.54	152	14688	282898	79446650
Quality of life decreased	59.68	15.54	32	14808	10388	79719160
Restlessness	55.45	15.54	55	14785	46437	79683111
Disorientation	53.25	15.54	62	14778	62714	79666834
Sepsis neonatal	51.55	15.54	9	14831	49	79729499
Loss of consciousness	51.27	15.54	103	14737	167840	79561708
Agitation	51.24	15.54	77	14763	99638	79629910
Malignant neoplasm progression	49.63	15.54	90	14750	135900	79593648
Polyneuropathy in malignant disease	47.62	15.54	11	14829	277	79729271
Tremor	46.85	15.54	100	14740	169983	79559565
Miosis	40.36	15.54	29	14811	15760	79713788
Reflexes abnormal	38.88	15.54	12	14828	931	79728617
Drug screen positive	35.79	15.54	19	14821	6044	79723504
Eyelid skin dryness	34.50	15.54	8	14832	205	79729343
Hypertensive crisis	33.33	15.54	29	14811	20741	79708807
Drug withdrawal syndrome neonatal	31.70	15.54	8	14832	295	79729253
Unresponsive to stimuli	31.42	15.54	45	14795	55743	79673805
Completed suicide	30.67	15.54	108	14732	245659	79483889
Depressed level of consciousness	29.13	15.54	59	14781	96593	79632955
Application site injury	28.99	15.54	5	14835	25	79729523
Hallucination	26.63	15.54	53	14787	85692	79643856
Sedation	26.54	15.54	40	14800	51855	79677693
Renal cell carcinoma stage I	26.44	15.54	5	14835	45	79729503
Amnestic disorder	25.98	15.54	8	14832	616	79728932
Xanthelasma	25.47	15.54	6	14834	165	79729383
Withdrawal syndrome	25.27	15.54	28	14812	26826	79702722
False positive investigation result	25.16	15.54	9	14831	1103	79728445
Product prescribing error	25.02	15.54	36	14804	44777	79684771
Chemical burn of oral cavity	24.62	15.54	5	14835	67	79729481
Drug dependence	24.61	15.54	34	14806	40735	79688813
Disturbance in attention	24.35	15.54	38	14802	50763	79678785
Tender joint count	24.27	15.54	6	14834	203	79729345
Hallucination, visual	23.94	15.54	30	14810	32699	79696849
Seizure	23.56	15.54	83	14757	188751	79540797
Pneumonia aspiration	22.75	15.54	43	14797	66924	79662624
Substance abuse	21.70	15.54	17	14823	10509	79719039
Psychomotor skills impaired	21.66	15.54	13	14827	5224	79724324
Application site ulcer	21.64	15.54	5	14835	126	79729422
Clubbing	20.88	15.54	7	14833	708	79728840
Hyperhidrosis	20.12	15.54	68	14772	151424	79578124
Asthenia	20.00	15.54	163	14677	511526	79218022
Mydriasis	19.43	15.54	20	14820	17623	79711925
Bradyphrenia	19.42	15.54	16	14824	10624	79718924
Pharyngeal enanthema	19.34	15.54	4	14836	59	79729489
Hyperresponsive to stimuli	19.16	15.54	4	14836	62	79729486
Thoracic vertebral fracture	19.07	15.54	12	14828	5241	79724307
Urinary retention	18.79	15.54	36	14804	56594	79672954
Embolism venous	18.78	15.54	11	14829	4228	79725320
Nausea	18.65	15.54	265	14575	956931	78772617
Synovectomy	18.45	15.54	5	14835	244	79729304
Joint swelling	18.39	15.54	16	14824	288630	79440918
Psychomotor hyperactivity	18.38	15.54	19	14821	16830	79712718
Suicidal ideation	17.76	15.54	42	14798	76298	79653250
Haemoglobin decreased	17.18	15.54	10	14830	222109	79507439
Alopecia	17.08	15.54	11	14829	231344	79498204
Myoclonic epilepsy	17.03	15.54	8	14832	1962	79727586
Synovial disorder	16.98	15.54	8	14832	1975	79727573
Bacteriuria	16.95	15.54	7	14833	1264	79728284
Application site erythema	16.89	15.54	11	14829	5099	79724449
Off label use	16.62	15.54	100	14740	907115	78822433
Gaze palsy	16.57	15.54	9	14831	2996	79726552
Application site reaction	16.51	15.54	6	14834	770	79728778
Benign prostatic hyperplasia	16.23	15.54	15	14825	11597	79717951
Clonus	16.20	15.54	12	14828	6828	79722720
Infection	15.88	15.54	13	14827	241699	79487849
Metastases to bone	15.69	15.54	21	14819	24406	79705142
Infusion related reaction	15.61	15.54	12	14828	230225	79499323
Radiculopathy	15.54	15.54	13	14827	8811	79720737

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N02AX06	NERVOUS SYSTEM ANALGESICS OPIOIDS Other opioids
FDA MoA	N0000000174	Opioid Agonists
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018759	Adrenergic Uptake Inhibitors
MeSH PA	D000700	Analgesics
MeSH PA	D000701	Analgesics, Opioid
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D009294	Narcotics
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D014179	Neurotransmitter Uptake Inhibitors
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
FDA EPC	N0000175690	Opioid Agonist

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

Disease	Relation	SNOMED_ID	DOID
Pain	indication	22253000
Chronic obstructive lung disease	contraindication	13645005	DOID:3083
Asthenia	contraindication	13791008
Alcohol intoxication	contraindication	25702006
Hypercapnia	contraindication	29596007
Myxedema	contraindication	43153006	DOID:11634
Paralytic ileus	contraindication	55525008	DOID:8442
Substance abuse	contraindication	66214007
Benign intracranial hypertension	contraindication	68267002	DOID:11459
Sleep apnea	contraindication	73430006	DOID:0050847
Pancreatitis	contraindication	75694006	DOID:4989
Decreased respiratory function	contraindication	80954004
Injury of head	contraindication	82271004
Cor pulmonale	contraindication	83291003	DOID:8515
Disorder of biliary tract	contraindication	105997008	DOID:9741
Seizure disorder	contraindication	128613002
Disease of liver	contraindication	235856003	DOID:409
Morbid obesity	contraindication	238136002	DOID:11981
Exacerbation of asthma	contraindication	281239006
Lesion of brain	contraindication	301766008
Coma	contraindication	371632003
Hypoxia	contraindication	389086002
Central nervous system depression	contraindication	418072004
Acute exacerbation of asthma	contraindication	708038006
Kyphoscoliosis with Respiratory Compromise	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.76	acidic
pKa2	9.12	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 100MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8309060	Nov. 20, 2023	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 100MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8309060	Nov. 20, 2023	RELIEF OF MODERATE TO SEVERE CHRONIC PAIN
EQ 150MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8309060	Nov. 20, 2023	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 150MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8309060	Nov. 20, 2023	RELIEF OF MODERATE TO SEVERE CHRONIC PAIN
EQ 200MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8309060	Nov. 20, 2023	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 200MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8309060	Nov. 20, 2023	RELIEF OF MODERATE TO SEVERE CHRONIC PAIN
EQ 250MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8309060	Nov. 20, 2023	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 250MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8309060	Nov. 20, 2023	RELIEF OF MODERATE TO SEVERE CHRONIC PAIN
EQ 50MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8309060	Nov. 20, 2023	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 50MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8309060	Nov. 20, 2023	RELIEF OF MODERATE TO SEVERE CHRONIC PAIN
EQ 100MG BASE	NUCYNTA	COLLEGIUM PHARM INC	N022304	Nov. 20, 2008	RX	TABLET	ORAL	7994364	June 27, 2025	RELIEF OF MODERATE TO SEVERE ACUTE PAIN
EQ 50MG BASE	NUCYNTA	COLLEGIUM PHARM INC	N022304	Nov. 20, 2008	RX	TABLET	ORAL	7994364	June 27, 2025	RELIEF OF MODERATE TO SEVERE ACUTE PAIN
EQ 75MG BASE	NUCYNTA	COLLEGIUM PHARM INC	N022304	Nov. 20, 2008	RX	TABLET	ORAL	7994364	June 27, 2025	RELIEF OF MODERATE TO SEVERE ACUTE PAIN
EQ 100MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	7994364	June 27, 2025	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 100MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	7994364	June 27, 2025	RELIEF OF MODERATE TO SEVERE CHRONIC PAIN
EQ 150MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	7994364	June 27, 2025	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 150MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	7994364	June 27, 2025	RELIEF OF MODERATE TO SEVERE CHRONIC PAIN
EQ 200MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	7994364	June 27, 2025	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 200MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	7994364	June 27, 2025	RELIEF OF MODERATE TO SEVERE CHRONIC PAIN
EQ 250MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	7994364	June 27, 2025	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 250MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	7994364	June 27, 2025	RELIEF OF MODERATE TO SEVERE CHRONIC PAIN
EQ 50MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	7994364	June 27, 2025	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 50MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	7994364	June 27, 2025	RELIEF OF MODERATE TO SEVERE CHRONIC PAIN
EQ 20MG BASE/ML	NUCYNTA	COLLEGIUM PHARM INC	N203794	Oct. 15, 2012	DISCN	SOLUTION	ORAL	7994364	June 27, 2025	MANAGEMENT OF MODERATE TO SEVERE ACUTE PAIN
EQ 100MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	11344512	April 21, 2028	A METHOD OF TITRATING AN OPIOID TO MANAGE NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 100MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	11344512	April 21, 2028	A METHOD OF TITRATING AN OPIOID TO MANAGE PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENTS ARE INADEQUATE
EQ 150MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	11344512	April 21, 2028	A METHOD OF TITRATING AN OPIOID TO MANAGE NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 150MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	11344512	April 21, 2028	A METHOD OF TITRATING AN OPIOID TO MANAGE PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENTS ARE INADEQUATE
EQ 200MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	11344512	April 21, 2028	A METHOD OF TITRATING AN OPIOID TO MANAGE NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 200MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	11344512	April 21, 2028	A METHOD OF TITRATING AN OPIOID TO MANAGE PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENTS ARE INADEQUATE
EQ 250MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	11344512	April 21, 2028	A METHOD OF TITRATING AN OPIOID TO MANAGE NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 250MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	11344512	April 21, 2028	A METHOD OF TITRATING AN OPIOID TO MANAGE PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENTS ARE INADEQUATE
EQ 50MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	11344512	April 21, 2028	A METHOD OF TITRATING AN OPIOID TO MANAGE NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 50MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	11344512	April 21, 2028	A METHOD OF TITRATING AN OPIOID TO MANAGE PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENTS ARE INADEQUATE
EQ 100MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8536130	Sept. 22, 2028	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 150MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8536130	Sept. 22, 2028	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 200MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8536130	Sept. 22, 2028	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 250MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8536130	Sept. 22, 2028	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 50MG BASE	NUCYNTA ER	COLLEGIUM PHARM INC	N200533	Aug. 25, 2011	RX	TABLET, EXTENDED RELEASE	ORAL	8536130	Sept. 22, 2028	MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 100MG BASE	NUCYNTA	COLLEGIUM PHARM INC	N022304	Nov. 20, 2008	RX	TABLET	ORAL	July 3, 2026	NEW PATIENT POPULATION
EQ 50MG BASE	NUCYNTA	COLLEGIUM PHARM INC	N022304	Nov. 20, 2008	RX	TABLET	ORAL	July 3, 2026	NEW PATIENT POPULATION
EQ 75MG BASE	NUCYNTA	COLLEGIUM PHARM INC	N022304	Nov. 20, 2008	RX	TABLET	ORAL	July 3, 2026	NEW PATIENT POPULATION
EQ 20MG BASE/ML	NUCYNTA	COLLEGIUM PHARM INC	N203794	Oct. 15, 2012	DISCN	SOLUTION	ORAL	July 3, 2026	NEW PATIENT POPULATION

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST	Ki	7.02	WOMBAT-PK	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	INHIBITOR	Ki	6.32	WOMBAT-PK	CHEMBL
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.66	CHEMBL

External reference:

ID	Source
4029061	VUID
N0000179820	NUI
D06007	KEGG_DRUG
4029061	VANDF
4029062	VANDF
C2001271	UMLSCUI
CHEBI:135935	CHEBI
CHEMBL1201776	ChEMBL_ID
CHEMBL1201777	ChEMBL_ID
D000077432	MESH_DESCRIPTOR_UI
DB06204	DRUGBANK_ID
7477	IUPHAR_LIGAND_ID
8216	INN_ID
H8A007M585	UNII
9838022	PUBCHEM_CID
787390	RXNORM
165888	MMSL
26545	MMSL
35753	MMSL
d07453	MMSL
013168	NDDF
013169	NDDF
441757005	SNOMEDCT_US
442004000	SNOMEDCT_US
442699004	SNOMEDCT_US
175591-23-8	SECONDARY_CAS_RN

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
NUCYNTA	HUMAN PRESCRIPTION DRUG LABEL	1	16590-289	TABLET, FILM COATED	100 mg	ORAL	NDA	35 sections
NUCYNTA	HUMAN PRESCRIPTION DRUG LABEL	1	16590-863	TABLET, FILM COATED	50 mg	ORAL	NDA	35 sections
NUCYNTA	HUMAN PRESCRIPTION DRUG LABEL	1	16590-889	TABLET, FILM COATED	75 mg	ORAL	NDA	32 sections
NUCYNTA	HUMAN PRESCRIPTION DRUG LABEL	1	21695-069	TABLET, FILM COATED	50 mg	ORAL	NDA	34 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	24510-050	TABLET, FILM COATED	50 mg	ORAL	NDA	39 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	24510-050	TABLET, FILM COATED	50 mg	ORAL	NDA	39 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	24510-058	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	38 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	24510-058	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	38 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	24510-075	TABLET, FILM COATED	75 mg	ORAL	NDA	39 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	24510-075	TABLET, FILM COATED	75 mg	ORAL	NDA	39 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	24510-100	TABLET, FILM COATED	100 mg	ORAL	NDA	39 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	24510-100	TABLET, FILM COATED	100 mg	ORAL	NDA	39 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	24510-116	TABLET, FILM COATED, EXTENDED RELEASE	100 mg	ORAL	NDA	38 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	24510-116	TABLET, FILM COATED, EXTENDED RELEASE	100 mg	ORAL	NDA	38 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	24510-174	TABLET, FILM COATED, EXTENDED RELEASE	150 mg	ORAL	NDA	38 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	24510-174	TABLET, FILM COATED, EXTENDED RELEASE	150 mg	ORAL	NDA	38 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	24510-232	TABLET, FILM COATED, EXTENDED RELEASE	200 mg	ORAL	NDA	38 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	24510-232	TABLET, FILM COATED, EXTENDED RELEASE	200 mg	ORAL	NDA	38 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	24510-291	TABLET, FILM COATED, EXTENDED RELEASE	250 mg	ORAL	NDA	38 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	24510-291	TABLET, FILM COATED, EXTENDED RELEASE	250 mg	ORAL	NDA	38 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5979	TABLET, FILM COATED	50 mg	ORAL	NDA	33 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	54868-6002	TABLET, FILM COATED	75 mg	ORAL	NDA	33 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	54868-6039	TABLET, FILM COATED	100 mg	ORAL	NDA	33 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	55700-792	TABLET, FILM COATED	50 mg	ORAL	NDA	37 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	55700-796	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	38 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	55700-797	TABLET, FILM COATED, EXTENDED RELEASE	100 mg	ORAL	NDA	38 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	69865-210	TABLET, FILM COATED	50 mg	ORAL	NDA	35 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	69865-220	TABLET, FILM COATED	75 mg	ORAL	NDA	35 sections
Nucynta	HUMAN PRESCRIPTION DRUG LABEL	1	69865-230	TABLET, FILM COATED	100 mg	ORAL	NDA	35 sections
NucyntaER	HUMAN PRESCRIPTION DRUG LABEL	1	69865-240	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	34 sections