Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
phosphodiesterase IV (PDE IV) inhibitors	3531	162401-32-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: libertek roflumilast daxas daliresp BY217 B9302-107 BYK20869	Roflumilast and its active metabolite (roflumilast N-oxide) are selective inhibitors of phosphodiesterase 4 (PDE4). Roflumilast and roflumilast N-oxide inhibition of PDE4 (a major cyclic-3′,5′-adenosine monophosphate (cyclic AMP)-metabolizing enzyme in lung tissue) activity leads to accumulation of intracellular cyclic AMP. While the specific mechanism(s) by which DALIRESP exerts its therapeutic action in COPD patients is not well defined, it is thought to be related to the effects of increased intracellular cyclic AMP in lung cells. Molecular weight: 403.21 Formula: C17H14Cl2F2N2O3 CLOGP: 3.12 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 60.45 ALOGS: -4.81 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

libertek
roflumilast
daxas
daliresp
BY217
B9302-107
BYK20869

Roflumilast and its active metabolite (roflumilast N-oxide) are selective inhibitors of phosphodiesterase 4 (PDE4). Roflumilast and roflumilast N-oxide inhibition of PDE4 (a major cyclic-3′,5′-adenosine monophosphate (cyclic AMP)-metabolizing enzyme in lung tissue) activity leads to accumulation of intracellular cyclic AMP. While the specific mechanism(s) by which DALIRESP exerts its therapeutic action in COPD patients is not well defined, it is thought to be related to the effects of increased intracellular cyclic AMP in lung cells.

Molecular weight: 403.21
Formula: C17H14Cl2F2N2O3
CLOGP: 3.12
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 60.45
ALOGS: -4.81
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.50	mg	O

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	1.92 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.20 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	15.10 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	80.50 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	3.748		Moderate	0.76
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.857		Moderate	0.76
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	44.566	10^-6 cm/s	Moderate	0.76
dh-clint	Dog hepatocyte intrinsic clearance	20.324	uL/min/10^6 cells	Moderate	0.76
dppb	Dog plasma protein binding (% unbound)	0.920	%	Moderate	0.76
fcs-ppb	Fetal calf serum protein binding (% unbound)	2.600	%	Moderate	0.76
herg	hERG pIC50	5.100	pIC50	Moderate	0.76
hh-clint	Human hepatocyte intrinsic clearance	9.268	uL/min/10^6 cells	Moderate	0.76
hlm-clint	Human liver microsomal intrinsic clearance	75.509	uL/min/mg protein	Moderate	0.76
hppb	Human plasma protein binding (% unbound)	0.610	%	Moderate	0.76
kinase-safety-class	ACVR2B,CAMK2D,EIF2AK3,GRK2,ITK,MAPK10,PDK1,PDK2,PDK4	9
kinase-selectivity-class	AXL,PDK1,PDK4	3
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	1.086		Moderate	0.76
mh-clint	Mouse hepatocyte intrinsic clearance	79.068		Moderate	0.76
mppb	Mouse plasma protein binding (% unbound)	1.210		Moderate	0.76
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	3.412		Moderate	0.76
pfas-class	PFAS structural alert (1 = True, 0 = False)	1
pppb	Pig plasma protein binding (% unbound)	2.230	%	Moderate	0.76
rh-clint	Rat hepatocyte intrinsic clearance	58.749	uL/min/10^6 cells	Moderate	0.76
rh-fuinc	Rat hepatocyte fraction unbound in incubation	15.790	%	Moderate	0.76
rppb	Rat plasma protein binding (% unbound)	0.750	%	Moderate	0.76
solubility-dd	Solubility at pH 7.4 in DMSO	3.041	uM	Moderate	0.76

Approvals:

Date	Agency	Company	Orphan
Feb. 28, 2011	EMA
Feb. 28, 2011	FDA	ASTRAZENECA 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
Chronic obstructive pulmonary disease	234.48	20.77	111	6294	73718	90548324
Dyspnoea	137.73	20.77	232	6173	880723	89741319
Full blood count abnormal	109.85	20.77	53	6352	36544	90585498
Asthma	106.87	20.77	107	6298	242053	90379989
Bronchial wall thickening	82.88	20.77	21	6384	2110	90619932
Bacterial disease carrier	80.60	20.77	20	6385	1846	90620196
Obstructive airways disorder	73.21	20.77	36	6369	25833	90596209
Bronchial secretion retention	71.88	20.77	21	6384	3594	90618448
Pneumothorax spontaneous	71.75	20.77	16	6389	929	90621113
Wheezing	71.51	20.77	86	6319	237994	90384048
Sleep disorder due to a general medical condition	67.33	20.77	41	6364	44697	90577345
Emphysema	67.00	20.77	27	6378	12128	90609914
Productive cough	66.46	20.77	50	6355	77013	90545029
Spinal cord compression	61.46	20.77	20	6385	4891	90617151
Cough	59.57	20.77	99	6306	368863	90253179
Pneumonia	57.66	20.77	134	6271	637925	89984117
Sputum discoloured	56.57	20.77	28	6377	20363	90601679
Adenocarcinoma	52.41	20.77	16	6389	3180	90618862
Hypercapnia	51.71	20.77	19	6386	6658	90615384
Death	50.39	20.77	104	6301	456447	90165595
Therapeutic product effect incomplete	48.54	20.77	64	6341	193832	90428210
Respiratory tract infection	47.98	20.77	37	6368	59041	90563001
Wrist fracture	47.98	20.77	23	6382	15601	90606441
Polymyalgia rheumatica	45.45	20.77	16	6389	4961	90617081
Multiple allergies	42.61	20.77	21	6384	15125	90606917
Breath sounds abnormal	42.29	20.77	21	6384	15365	90606677
Rales	38.82	20.77	20	6385	15807	90606235
Intervertebral disc protrusion	38.55	20.77	24	6381	27172	90594870
Upper limb fracture	38.28	20.77	22	6383	21556	90600486
Weight decreased	37.77	20.77	83	6322	379827	90242215
Microstomia	32.15	20.77	5	6400	37	90622005
Spirometry abnormal	28.42	20.77	6	6399	269	90621773
Eosinophilia	27.93	20.77	20	6385	28513	90593529
Lung diffusion disorder	26.74	20.77	5	6400	119	90621923
Dermatitis atopic	26.60	20.77	18	6387	23454	90598588
Pneumonitis	26.09	20.77	23	6382	44147	90577895
Influenza	26.00	20.77	40	6365	139224	90482818
Hyperthyroidism	25.55	20.77	16	6389	18294	90603748
Disease recurrence	25.07	20.77	21	6384	37632	90584410
Alopecia	24.70	20.77	3	6402	495068	90126974
Poor venous access	24.60	20.77	16	6389	19511	90602531
Diarrhoea	23.40	20.77	129	6276	939061	89682981
Lung hernia	21.28	20.77	3	6402	10	90622032
Suicidal ideation	21.00	20.77	26	6379	73829	90548213

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
Dyspnoea	209.79	24.47	261	4906	442360	42173808
Chronic obstructive pulmonary disease	202.71	24.47	114	5053	63000	42553168
Asthma	89.33	24.47	68	5099	62246	42553922
Product prescribing error	80.45	24.47	46	5121	26066	42590102
Asthma-chronic obstructive pulmonary disease overlap syndrome	78.15	24.47	21	5146	1538	42614630
Wheezing	76.78	24.47	59	5108	54722	42561446
Weight decreased	75.01	24.47	108	5059	207840	42408328
Sputum discoloured	63.99	24.47	29	5138	10103	42606065
Cough	61.97	24.47	91	5076	178012	42438156
Emphysema	53.74	24.47	27	5140	11808	42604360
Pulmonary mass	45.69	24.47	27	5140	16238	42599930
Sinus pain	44.15	24.47	12	5155	917	42615251
Death	43.30	24.47	140	5027	471045	42145123
Nasal obstruction	43.26	24.47	12	5155	989	42615179
Suicidal ideation	37.25	24.47	37	5130	48124	42568044
Insomnia	34.81	24.47	56	5111	118197	42497971
Diarrhoea	34.50	24.47	128	5039	460721	42155447
Chest discomfort	33.66	24.47	40	5127	63576	42552592
Bronchiectasis	33.37	24.47	23	5144	17996	42598172
Decreased appetite	31.40	24.47	71	5096	193066	42423102
Obstructive airways disorder	31.04	24.47	25	5142	24734	42591434
Mycobacterium avium complex infection	30.23	24.47	12	5155	3015	42613153
Pneumonia	28.87	24.47	114	5053	422035	42194133
Pulmonary function test decreased	28.76	24.47	14	5153	5718	42610450
Osteopenia	27.55	24.47	14	5153	6264	42609904
Oedema peripheral	26.67	24.47	54	5113	136022	42480146
Cold sweat	24.68	24.47	16	5151	11314	42604854

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
Chronic obstructive pulmonary disease	344.58	22.43	172	9020	108986	110471121
Dyspnoea	285.14	22.43	400	8792	1106472	109473635
Asthma	154.28	22.43	143	9049	250148	110329959
Full blood count abnormal	121.86	22.43	69	9123	55983	110524124
Sputum discoloured	112.10	22.43	52	9140	27893	110552214
Cough	99.11	22.43	154	9038	461487	110118620
Wheezing	94.34	22.43	111	9081	255119	110324988
Emphysema	83.10	22.43	38	9154	19718	110560389
Product prescribing error	82.41	22.43	52	9140	51279	110528828
Weight decreased	80.04	22.43	141	9051	467916	110112191
Bronchial wall thickening	79.82	22.43	23	9169	3184	110576923
Sleep disorder due to a general medical condition	79.21	22.43	51	9141	52061	110528046
Bacterial disease carrier	78.18	22.43	21	9171	2248	110577859
Obstructive airways disorder	74.71	22.43	47	9145	46102	110534005
Pneumonia	68.65	22.43	193	8999	876521	109703586
Productive cough	67.74	22.43	64	9128	114241	110465866
Bronchial secretion retention	61.71	22.43	21	9171	5003	110575104
Therapeutic product effect incomplete	59.96	22.43	83	9109	223722	110356385
Pneumothorax spontaneous	58.77	22.43	16	9176	1801	110578306
Death	51.81	22.43	151	9041	698718	109881389
Respiratory tract infection	50.05	22.43	44	9148	71573	110508534
Spinal cord compression	49.88	22.43	20	9172	7532	110572575
Wrist fracture	49.16	22.43	24	9168	14393	110565714
Adenocarcinoma	45.27	22.43	16	9176	4264	110575843
Hypercapnia	39.32	22.43	19	9173	11140	110568967
Polymyalgia rheumatica	38.90	22.43	16	9176	6426	110573681
Multiple allergies	37.62	22.43	19	9173	12244	110567863
Breath sounds abnormal	36.47	22.43	24	9168	25380	110554727
Suicidal ideation	34.86	22.43	41	9151	93896	110486211
Intervertebral disc protrusion	34.59	22.43	24	9168	27674	110552433
Upper limb fracture	33.11	22.43	21	9171	20867	110559240
Decreased appetite	31.58	22.43	99	9093	475747	110104360
Microstomia	31.22	22.43	5	9187	38	110580069
Rales	29.87	22.43	21	9171	24718	110555389
Pulmonary mass	28.24	22.43	24	9168	37277	110542830
Mycobacterium avium complex infection	26.91	22.43	12	9180	5865	110574242
Haematochezia	26.73	22.43	40	9152	115484	110464623
Toxicity to various agents	24.62	22.43	5	9187	480550	110099557
Cold sweat	22.72	22.43	17	9175	22014	110558093
Dermatitis atopic	22.61	22.43	18	9174	25523	110554584
Nasal obstruction	22.56	22.43	9	9183	3341	110576766

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	D05AX06	DERMATOLOGICALS ANTIPSORIATICS ANTIPSORIATICS FOR TOPICAL USE Other antipsoriatics for topical use
ATC	R03DX07	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES Other systemic drugs for obstructive airway diseases
FDA MoA	N0000182960	Phosphodiesterase 4 Inhibitors
FDA EPC	N0000182961	Phosphodiesterase 4 Inhibitor
CHEBI has role	CHEBI:35469	antidepressant
CHEBI has role	CHEBI:35476	antipsychotic agent
CHEBI has role	CHEBI:35526	hypoglycemic agent
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:49167	anti-asthmatic drug
CHEBI has role	CHEBI:50177	dermatologic drug
CHEBI has role	CHEBI:50748	antipsoriatic
CHEBI has role	CHEBI:65023	anti-asthmatic agent
CHEBI has role	CHEBI:68844	phosphodiesterase IV inhibitor
CHEBI has role	CHEBI:74518	anti-obesity agent

Related Drugs by ATC class:

D05AX Other antipsoriatics for topical use 7 drugs

calcipotriene calcitriol fumaric acid tacalcitol tapinarof tazarotene ulobetasol propionate

R03DX Other systemic drugs for obstructive airway diseases 10 drugs

amlexanox benralizumab depemokimab-ulaa eprozinol fenspiride mepolizumab omalizumab reslizumab seratrodast tezepelumab

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

Disease	Relation	SNOMED_ID	DOID
Seborrheic dermatitis	indication	50563003	DOID:8741
Plaque psoriasis	indication	200965009
Severe chronic obstructive pulmonary disease	indication	313299006
COPD Associated with Chronic Bronchitis	indication
Suicidal thoughts	contraindication	6471006
Mood swings	contraindication	18963009
Depressive disorder	contraindication	35489007
Hepatic failure	contraindication	59927004
Weight loss	contraindication	89362005
Suicidal	contraindication	267073005

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.92	acidic
pKa2	2.32	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
0.05%	ZORYVE	ARCUTIS	N215985	Oct. 4, 2025	RX	CREAM	TOPICAL	11819496	June 7, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS IN PEDIATRIC PATIENTS 2 TO 5 YEARS OF AGE
0.05%	ZORYVE	ARCUTIS	N215985	Oct. 4, 2025	RX	CREAM	TOPICAL	11992480	June 7, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS IN PEDIATRIC PATIENTS 2 TO 5 YEARS OF AGE
0.05%	ZORYVE	ARCUTIS	N215985	Oct. 4, 2025	RX	CREAM	TOPICAL	12005051	June 7, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS IN PEDIATRIC PATIENTS 2 TO 5 YEARS OF AGE
0.05%	ZORYVE	ARCUTIS	N215985	Oct. 4, 2025	RX	CREAM	TOPICAL	12310956	June 7, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS IN PEDIATRIC PATIENTS 2 TO 5 YEARS OF AGE
0.05%	ZORYVE	ARCUTIS	N215985	Oct. 4, 2025	RX	CREAM	TOPICAL	9907788	June 7, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS IN PEDIATRIC PATIENTS 2 TO 5 YEARS OF AGE
0.15%	ZORYVE	ARCUTIS	N215985	July 9, 2024	RX	CREAM	TOPICAL	11819496	June 7, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS
0.15%	ZORYVE	ARCUTIS	N215985	July 9, 2024	RX	CREAM	TOPICAL	11992480	June 7, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS
0.15%	ZORYVE	ARCUTIS	N215985	July 9, 2024	RX	CREAM	TOPICAL	12005051	June 7, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS
0.15%	ZORYVE	ARCUTIS	N215985	July 9, 2024	RX	CREAM	TOPICAL	12310956	June 7, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS
0.15%	ZORYVE	ARCUTIS	N215985	July 9, 2024	RX	CREAM	TOPICAL	9907788	June 7, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS
0.3%	ZORYVE	ARCUTIS	N215985	July 29, 2022	RX	CREAM	TOPICAL	11819496	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS, INCLUDING INTERTRIGINOUS AREAS, IN PATIENTS 6 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N215985	July 29, 2022	RX	CREAM	TOPICAL	11992480	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS, INCLUDING INTERTRIGINOUS AREAS, IN PATIENTS 6 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N215985	July 29, 2022	RX	CREAM	TOPICAL	12005051	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS, INCLUDING INTERTRIGINOUS AREAS, IN PATIENTS 6 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N215985	July 29, 2022	RX	CREAM	TOPICAL	12310956	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS, INCLUDING INTERTRIGINOUS AREAS, IN PATIENTS 6 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N215985	July 29, 2022	RX	CREAM	TOPICAL	9907788	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS, INCLUDING INTERTRIGINOUS AREAS, IN PATIENTS 12 YEARS OF AGE AND OLDER. (1)
0.3%	ZORYVE	ARCUTIS	N215985	July 29, 2022	RX	CREAM	TOPICAL	9907788	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS, INCLUDING INTERTRIGINOUS AREAS, IN PATIENTS 6 YEARS OF AGE OR OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	11819496	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS OF THE SCALP AND BODY IN PATIENTS 12 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	11819496	June 7, 2037	TOPICAL TREATMENT OF SEBORRHEIC DERMATITIS IN PATIENTS 9 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	11992480	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS OF THE SCALP AND BODY IN PATIENTS 12 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	11992480	June 7, 2037	TOPICAL TREATMENT OF SEBORRHEIC DERMATITIS IN PATIENTS 9 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	12005051	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS OF THE SCALP AND BODY IN PATIENTS 12 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	12005051	June 7, 2037	TOPICAL TREATMENT OF SEBORRHEIC DERMATITIS IN PATIENTS 9 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	12310956	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS OF THE SCALP AND BODY IN PATIENTS 12 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	12310956	June 7, 2037	TOPICAL TREATMENT OF SEBORRHEIC DERMATITIS IN PATIENTS 9 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	9907788	June 7, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS OF THE SCALP AND BODY IN PATIENTS 12 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	9907788	June 7, 2037	TOPICAL TREATMENT OF SEBORRHEIC DERMATITIS IN PATIENTS 9 YEARS OF AGE AND OLDER
0.05%	ZORYVE	ARCUTIS	N215985	Oct. 4, 2025	RX	CREAM	TOPICAL	11129818	Aug. 25, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS IN PEDIATRIC PATIENTS 2 TO 5 YEARS OF AGE
0.15%	ZORYVE	ARCUTIS	N215985	July 9, 2024	RX	CREAM	TOPICAL	11129818	Aug. 25, 2037	TOPICAL TREATMENT OF MILD TO MODERATE ATOPIC DERMATITIS
0.3%	ZORYVE	ARCUTIS	N215985	July 29, 2022	RX	CREAM	TOPICAL	11129818	Aug. 25, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS, INCLUDING INTERTRIGINOUS AREAS, IN PATIENTS 12 YEARS OF AGE AND OLDER. (1)
0.3%	ZORYVE	ARCUTIS	N215985	July 29, 2022	RX	CREAM	TOPICAL	11129818	Aug. 25, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS, INCLUDING INTERTRIGINOUS AREAS, IN PATIENTS 6 YEARS OF AGE OR OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	11129818	Aug. 25, 2037	TOPICAL TREATMENT OF PLAQUE PSORIASIS OF THE SCALP AND BODY IN PATIENTS 12 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	11129818	Aug. 25, 2037	TOPICAL TREATMENT OF SEBORRHEIC DERMATITIS IN PATIENTS 9 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	11707454	Dec. 3, 2041	TOPICAL TREATMENT OF SEBORRHEIC DERMATITIS IN PATIENTS 9 YEARS OF AGE AND OLDER
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	12329751	Dec. 3, 2041	TOPICAL TREATMENT OF SEBORRHEIC DERMATITIS IN PATIENTS 9 YEARS OF AGE AND OLDER

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
0.3%	ZORYVE	ARCUTIS	N215985	July 29, 2022	RX	CREAM	TOPICAL	Oct. 5, 2026	NEW PATIENT POPULATION
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	Dec. 15, 2026	NEW PRODUCT
0.15%	ZORYVE	ARCUTIS	N215985	July 9, 2024	RX	CREAM	TOPICAL	July 9, 2027	NEW STRENGTH
0.3%	ZORYVE	ARCUTIS	N217242	Dec. 15, 2023	RX	FOAM	TOPICAL	May 22, 2028	TREATMENT OF PLAQUE PSORIASIS OF THE SCALP AND BODY IN PATIENTS 12 YEARS OF AGE AND OLDER
0.05%	ZORYVE	ARCUTIS	N215985	Oct. 4, 2025	RX	CREAM	TOPICAL	Oct. 4, 2028	NEW STRENGTH

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Phosphodiesterase 4	Enzyme	P27815 Q07343 Q08493 Q08499	PDE4A_HUMAN PDE4B_HUMAN PDE4C_HUMAN PDE4D_HUMAN	INHIBITOR	IC50	9.10	CHEMBL	CHEMBL
cAMP-specific 3',5'-cyclic phosphodiesterase 4B	Enzyme	Q07343	PDE4B_HUMAN		IC50	9.40	CHEMBL
cAMP-specific 3',5'-cyclic phosphodiesterase 4A	Enzyme	P27815	PDE4A_HUMAN		IC50	9.46	CHEMBL
cAMP-specific 3',5'-cyclic phosphodiesterase 4D	Enzyme	Q08499	PDE4D_HUMAN		IC50	9.57	CHEMBL
Phosphodiesterase	Enzyme		Q8WQX9_9TRYP		Ki	5.50	CHEMBL

External reference:

ID	Source
4030722	VUID
N0000182732	NUI
D05744	KEGG_DRUG
4030722	VANDF
C0965618	UMLSCUI
CHEBI:47657	CHEBI
ROF	PDB_CHEM_ID
CHEMBL193240	ChEMBL_ID
DB01656	DRUGBANK_ID
C424423	MESH_SUPPLEMENTAL_RECORD_UI
449193	PUBCHEM_CID
6962	IUPHAR_LIGAND_ID
7598	INN_ID
0P6C6ZOP5U	UNII
1091836	RXNORM
180364	MMSL
27361	MMSL
358833	MMSL
399966	MMSL
d07684	MMSL
013499	NDDF
448971002	SNOMEDCT_US
714680006	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Daliresp	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0088	TABLET	250 ug	ORAL	NDA	27 sections
Daliresp	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0095	TABLET	500 ug	ORAL	NDA	27 sections
Roflumilast	Human Prescription Drug Label	1	0904-7399	TABLET	500 ug	ORAL	ANDA	25 sections
Roflumilast	Human Prescription Drug Label	1	0904-7399	TABLET	500 ug	ORAL	ANDA	25 sections
Roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7483	TABLET	500 ug	ORAL	ANDA	25 sections
Roflumilast	Human Prescription Drug Label	1	0904-7493	TABLET	250 ug	ORAL	ANDA	25 sections
Roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	31722-623	TABLET	500 ug	ORAL	ANDA	27 sections
Roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	31722-676	TABLET	250 ug	ORAL	ANDA	27 sections
ROFLUMILAST	HUMAN PRESCRIPTION DRUG LABEL	1	42571-259	TABLET	500 ug	ORAL	ANDA	26 sections
ROFLUMILAST	HUMAN PRESCRIPTION DRUG LABEL	1	42571-369	TABLET	250 ug	ORAL	ANDA	26 sections
ROFLUMILAST	HUMAN PRESCRIPTION DRUG LABEL	1	43547-005	TABLET	500 ug	ORAL	ANDA	19 sections
Roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	51407-975	TABLET	500 ug	ORAL	ANDA	24 sections
ROFLUMILAST	Human Prescription Drug Label	1	59651-275	TABLET	500 ug	ORAL	ANDA	26 sections
ROFLUMILAST	Human Prescription Drug Label	1	59651-801	TABLET	250 ug	ORAL	ANDA	26 sections
Roflumilast	Human Prescription Drug Label	1	59746-801	TABLET	250 ug	ORAL	ANDA	27 sections
Roflumilast	Human Prescription Drug Label	1	59746-802	TABLET	500 ug	ORAL	ANDA	27 sections
Roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	60687-786	TABLET	500 ug	ORAL	ANDA	27 sections
roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	64380-287	TABLET	250 ug	ORAL	ANDA	25 sections
roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	64380-786	TABLET	500 ug	ORAL	ANDA	25 sections
Roflumilast	Human Prescription Drug Label	1	67877-480	TABLET	500 ug	ORAL	ANDA	24 sections
Roflumilast	Human Prescription Drug Label	1	67877-730	TABLET	250 ug	ORAL	ANDA	24 sections
Roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	68382-624	TABLET	250 ug	ORAL	ANDA	25 sections
Roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	68382-969	TABLET	500 ug	ORAL	ANDA	25 sections
ROFLUMILAST	Human Prescription Drug Label	1	69292-630	TABLET	250 ug	ORAL	ANDA	27 sections
ROFLUMILAST	Human Prescription Drug Label	1	69292-631	TABLET	500 ug	ORAL	ANDA	27 sections
Roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	70771-1673	TABLET	250 ug	ORAL	ANDA	2 sections
Roflumilast	HUMAN PRESCRIPTION DRUG LABEL	1	70771-1674	TABLET	500 ug	ORAL	ANDA	2 sections
ROFLUMILAST	HUMAN PRESCRIPTION DRUG LABEL	1	72162-2385	TABLET	500 ug	ORAL	ANDA	26 sections
Roflumilast	Human Prescription Drug Label	1	72205-200	TABLET	500 ug	ORAL	ANDA	25 sections
Roflumilast	Human Prescription Drug Label	1	72205-201	TABLET	250 ug	ORAL	ANDA	25 sections

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roflumilast 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: