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

Stem definitionDrug idCAS RN
phosphodiesterase IV (PDE IV) inhibitors 3531 162401-32-3

Description:

MoleculeDescription

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:

DoseUnitRoute
0.50 mg O

ADMET properties:

PropertyValueReference
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):

PropertyDescriptionValueUnitConfidenceSimilarity
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:

DateAgencyCompanyOrphan
Feb. 28, 2011 EMA
Feb. 28, 2011 FDA ASTRAZENECA PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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
calcipotrienecalcitriolfumaric acidtacalcitoltapinaroftazaroteneulobetasol propionate
R03DX Other systemic drugs for obstructive airway diseases 10 drugs
amlexanoxbenralizumabdepemokimab-ulaaeprozinolfenspiridemepolizumabomalizumabreslizumabseratrodasttezepelumab

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

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 10.92 acidic
pKa2 2.32 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Phosphodiesterase 4 Enzyme INHIBITOR IC50 9.10 CHEMBL CHEMBL
cAMP-specific 3',5'-cyclic phosphodiesterase 4B Enzyme IC50 9.40 CHEMBL
cAMP-specific 3',5'-cyclic phosphodiesterase 4A Enzyme IC50 9.46 CHEMBL
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Enzyme IC50 9.57 CHEMBL
Phosphodiesterase Enzyme Ki 5.50 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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