apremilast Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
phosphodiesterase IV (PDE IV) inhibitors 4829 608141-41-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • apremilast
  • CC-10004
  • otezla
Apremilast is an oral small-molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels. The specific mechanism(s) by which apremilast exerts its therapeutic action in psoriatic arthritis patients and psoriasis patients is not well defined.
  • Molecular weight: 460.50
  • Formula: C22H24N2O7S
  • CLOGP: 1.46
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 1
  • TPSA: 119.08
  • ALOGS: -4.13
  • ROTB: 8

Drug dosage:

DoseUnitRoute
60 mg O

Approvals:

DateAgencyCompanyOrphan
Sept. 20, 2019 PMDA Celgene K.K.
March 21, 2014 FDA CELGENE CORP
Nov. 20, 2014 EMA

FDA Adverse Event Reporting System

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
Diarrhoea 32114.54 78.08 11606 48444 138579 4440363
Psoriasis 26304.96 78.08 6930 53120 23354 4555588
Nausea 25264.51 78.08 10230 49820 167103 4411839
Headache 20364.44 78.08 7942 52108 114431 4464511
Drug ineffective 10755.90 78.08 5823 54227 180238 4398704
Abdominal discomfort 9183.36 78.08 3047 57003 25361 4553581
Product dose omission 8560.90 78.08 3635 56415 63327 4515615
Psoriatic arthropathy 6445.36 78.08 1671 58379 4887 4574055
Depression 5016.55 78.08 2265 57785 45468 4533474
Adverse drug reaction 4310.42 78.08 1471 58579 13268 4565674
Weight decreased 4214.62 78.08 2094 57956 52370 4526572
Abdominal pain upper 3338.80 78.08 1557 58493 33558 4545384
Vomiting 2507.20 78.08 2008 58042 117691 4461251
Therapy non-responder 2270.10 78.08 941 59109 15036 4563906
Rash 2214.09 78.08 1793 58257 106595 4472347
Frequent bowel movements 1634.68 78.08 504 59546 3139 4575803
Arthralgia 1619.56 78.08 1332 58718 80662 4498280
Migraine 1568.46 78.08 693 59357 13016 4565926
Gastric disorder 1557.09 78.08 546 59504 5336 4573606
Insomnia 1499.11 78.08 1005 59045 44340 4534602
Decreased appetite 1423.90 78.08 1060 58990 55337 4523605
Pain 1327.22 78.08 1256 58794 91614 4487328
Fatigue 1294.55 78.08 1528 58522 144038 4434904
Dyspepsia 1267.29 78.08 628 59422 15426 4563516
Therapeutic product effect decreased 1260.30 78.08 658 59392 18095 4560847
Therapeutic response decreased 1253.73 78.08 603 59447 13848 4565094
Pruritus 1149.19 78.08 1040 59010 71532 4507410
Gastrointestinal disorder 1132.10 78.08 582 59468 15479 4563463
Malaise 1094.74 78.08 1116 58934 89041 4489901
Upper respiratory tract infection 1081.09 78.08 537 59513 13250 4565692
Nasopharyngitis 919.21 78.08 663 59387 32854 4546088
Dizziness 780.62 78.08 984 59066 98887 4480055
Muscle spasms 756.27 78.08 604 59446 34886 4544056
Memory impairment 740.36 78.08 480 59570 19923 4559019
Flatulence 717.75 78.08 344 59706 7820 4571122
Faeces soft 703.80 78.08 191 59859 690 4578252
Tension headache 696.90 78.08 188 59862 660 4578282
Stress 664.75 78.08 348 59702 9600 4569342
Sinusitis 660.80 78.08 466 59584 22246 4556696
Abdominal pain 599.72 78.08 671 59379 59353 4519589
Cough 585.69 78.08 639 59411 54948 4523994
Influenza 570.10 78.08 411 59639 20312 4558630
Gastrooesophageal reflux disease 517.19 78.08 341 59709 14552 4564390
Back pain 516.17 78.08 572 59478 50027 4528915
Unevaluable event 504.66 78.08 349 59701 16127 4562815
Alopecia 492.09 78.08 427 59623 27653 4551289
Anxiety 490.12 78.08 543 59507 47468 4531474
Arthropathy 489.94 78.08 292 59758 10406 4568536
Mood altered 484.13 78.08 230 59820 5119 4573823
Pain in extremity 470.20 78.08 611 59439 63128 4515814
Feeling abnormal 424.67 78.08 442 59608 35963 4542979
Peripheral swelling 422.07 78.08 383 59667 26309 4552633
Enthesopathy 413.10 78.08 100 59950 194 4578748
Therapeutic product effect incomplete 405.35 78.08 311 59739 16897 4562045
Arthritis 405.21 78.08 292 59758 14408 4564534
Rhinorrhoea 380.31 78.08 260 59790 11782 4567160
Bronchitis 365.72 78.08 312 59738 19728 4559214
Abdominal distension 346.63 78.08 289 59761 17700 4561242
Suicidal ideation 345.68 78.08 312 59738 21271 4557671
Treatment failure 329.48 78.08 254 59796 13893 4565049
Condition aggravated 329.04 78.08 491 59559 57680 4521262
Discomfort 321.07 78.08 203 59847 8047 4570895
Loss of personal independence in daily activities 301.91 78.08 194 59856 7911 4571031
Depressed mood 298.46 78.08 199 59851 8645 4570297
Drug intolerance 280.71 78.08 279 59771 21467 4557475
Dry skin 265.07 78.08 201 59849 10721 4568221
Tenosynovitis 250.04 78.08 86 59964 786 4578156
Skin exfoliation 243.76 78.08 191 59859 10696 4568246
Tremor 237.03 78.08 328 59722 35931 4543011
Rash pruritic 233.10 78.08 197 59853 12286 4566656
Musculoskeletal stiffness 230.16 78.08 235 59815 18667 4560275
Nasal congestion 228.41 78.08 182 59868 10444 4568498
Myalgia 227.78 78.08 348 59702 41700 4537242
Mood swings 221.42 78.08 139 59911 5438 4573504
Synovitis 220.62 78.08 119 59931 3486 4575456
Therapy cessation 212.01 78.08 162 59888 8738 4570204
Gastroenteritis viral 205.55 78.08 115 59935 3625 4575317
Joint swelling 198.09 78.08 244 59806 23834 4555108
Hypersensitivity 185.92 78.08 302 59748 38119 4540823
Sinus headache 181.44 78.08 76 59974 1239 4577703
Ear infection 180.60 78.08 117 59933 4836 4574106
Urinary tract infection 178.32 78.08 313 59737 42077 4536865
C-reactive protein abnormal 173.63 78.08 70 59980 1030 4577912
Therapy partial responder 166.75 78.08 63 59987 771 4578171
Infection 166.66 78.08 278 59772 35864 4543078
Constipation 155.41 78.08 294 59756 41860 4537082
Palpitations 153.74 78.08 219 59831 24627 4554315
Sinus disorder 151.24 78.08 95 59955 3719 4575223
Adverse event 144.61 78.08 171 59879 16001 4562941
Bowel movement irregularity 143.94 78.08 59 59991 908 4578034
Multiple allergies 143.47 78.08 63 59987 1159 4577783
Incorrect dose administered 142.86 78.08 186 59864 19199 4559743
Defaecation urgency 141.82 78.08 55 59995 726 4578216
Nephrolithiasis 141.36 78.08 129 59921 8910 4570032
Rebound psoriasis 137.53 78.08 31 60019 36 4578906
Respiratory tract infection 134.88 78.08 114 59936 7106 4571836
Irritable bowel syndrome 133.39 78.08 77 59973 2579 4576363
Toxicity to various agents 131.33 78.08 3 60047 72037 4506905
Skin discolouration 129.70 78.08 121 59929 8597 4570345
Rash macular 129.23 78.08 101 59949 5631 4573311
Rheumatoid arthritis 125.67 78.08 200 59850 24799 4554143
Irritability 124.53 78.08 144 59906 13155 4565787
Feeling jittery 124.14 78.08 77 59973 2947 4575995
Retching 121.50 78.08 80 59970 3399 4575543
Back disorder 120.14 78.08 72 59978 2588 4576354
Tendonitis 117.72 78.08 82 59968 3826 4575116
Skin fissures 117.20 78.08 65 59985 2013 4576929
Urticaria 116.04 78.08 251 59799 39322 4539620
Joint stiffness 114.53 78.08 96 59954 5915 4573027
Oropharyngeal pain 113.58 78.08 157 59893 17162 4561780
Gastrointestinal pain 109.65 78.08 59 59991 1719 4577223
Skin disorder 109.61 78.08 96 59954 6280 4572662
Blood pressure increased 107.96 78.08 205 59845 29255 4549687
Tongue disorder 106.70 78.08 58 59992 1725 4577217
Pregnancy 105.88 78.08 109 59941 8735 4570207
Seasonal allergy 103.65 78.08 63 59987 2324 4576618
Influenza like illness 102.88 78.08 158 59892 18995 4559947
Off label use 98.11 78.08 71 59979 129042 4449900
Adverse reaction 94.21 78.08 61 59989 2518 4576424
Eructation 94.05 78.08 55 59995 1888 4577054
Respiratory disorder 94.04 78.08 97 59953 7791 4571151
Nervousness 93.22 78.08 96 59954 7696 4571246
Gallbladder disorder 90.51 78.08 71 59979 3979 4574963
Asthenia 89.15 78.08 378 59672 85785 4493157
Diverticulitis 88.16 78.08 89 59961 6968 4571974
Crying 85.68 78.08 83 59967 6180 4572762
Acute kidney injury 85.39 78.08 19 60031 70412 4508530
Heart rate increased 84.58 78.08 142 59908 18400 4560542
Productive cough 81.61 78.08 98 59952 9315 4569627
Gout 81.58 78.08 69 59981 4304 4574638
Neutropenia 80.37 78.08 4 60046 47946 4530996
Pollakiuria 78.09 78.08 84 59966 7081 4571861

Pharmacologic Action:

SourceCodeDescription
ATC L04AA32 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory drug
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D018501 Antirheumatic Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Psoriasis with arthropathy indication 33339001
Plaque psoriasis indication 200965009
Beh├žet's disease affecting oral mucosa indication 403443000

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR INHIBITING PDE4
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7208516 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8802717 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR INHIBITING PDE4
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7208516 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8802717 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 6962940 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR INHIBITING PDE4
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7208516 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 7659302 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8455536 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 8802717 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9018243 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 TREATMENT OF PATIENTS WITH MODERATE TO SEVERE PLAQUE PSORIASIS WHO ARE CANDIDATES FOR PHOTOTHERAPY OR SYSTEMIC THERAPY
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIASIS
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9724330 March 19, 2023 USE OF OTEZLA (APREMILAST) FOR THE TREATMENT OF PSORIATIC ARTHRITIS
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 10092541 May 29, 2034 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE USING A DOSAGE TITRATION SCHEDULE
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 10092541 May 29, 2034 TREATMENT OF PSORIASIS USING A DOSAGE TITRATION SCHEDULE
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9872854 May 29, 2034 TREATMENT OF PSORIATIC ARTHRITIS USING A DOSAGE TITRATION SCHEDULE
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9872854 May 29, 2034 TREATMENT OF PSORIATIC ARTHRITIS WITH APREMILAST USING A DOSAGE TITRATION SCHEDULE AND A SECOND ACTIVE AGENT
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 10092541 May 29, 2034 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE USING A DOSAGE TITRATION SCHEDULE
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 10092541 May 29, 2034 TREATMENT OF PSORIASIS USING A DOSAGE TITRATION SCHEDULE
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9872854 May 29, 2034 TREATMENT OF PSORIATIC ARTHRITIS USING A DOSAGE TITRATION SCHEDULE
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9872854 May 29, 2034 TREATMENT OF PSORIATIC ARTHRITIS WITH APREMILAST USING A DOSAGE TITRATION SCHEDULE AND A SECOND ACTIVE AGENT
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 10092541 May 29, 2034 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCET'S DISEASE USING A DOSAGE TITRATION SCHEDULE
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 10092541 May 29, 2034 TREATMENT OF PSORIASIS USING A DOSAGE TITRATION SCHEDULE
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9872854 May 29, 2034 TREATMENT OF PSORIATIC ARTHRITIS USING A DOSAGE TITRATION SCHEDULE
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL 9872854 May 29, 2034 TREATMENT OF PSORIATIC ARTHRITIS WITH APREMILAST USING A DOSAGE TITRATION SCHEDULE AND A SECOND ACTIVE AGENT

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL July 19, 2022 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCETS DISEASE
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL July 19, 2022 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCETS DISEASE
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL July 19, 2022 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCETS DISEASE
10MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL July 19, 2026 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCETS DISEASE
20MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL July 19, 2026 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCETS DISEASE
30MG OTEZLA AMGEN INC N205437 March 21, 2014 RX TABLET ORAL July 19, 2026 TREATMENT OF ADULT PATIENTS WITH ORAL ULCERS ASSOCIATED WITH BEHCETS DISEASE

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Enzyme INHIBITOR IC50 7.13 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
cAMP-specific 3',5'-cyclic phosphodiesterase 4A Enzyme INHIBITOR IC50 7.85 IUPHAR
cAMP-specific 3',5'-cyclic phosphodiesterase 4C Enzyme INHIBITOR IC50 6.93 IUPHAR
cAMP-specific 3',5'-cyclic phosphodiesterase 4B Enzyme INHIBITOR IC50 7.57 IUPHAR

External reference:

IDSource
D08860 KEGG_DRUG
4033216 VUID
N0000190644 NUI
C1678805 UMLSCUI
714684002 SNOMEDCT_US
1492727 RXNORM
015411 NDDF
30225 MMSL
d08247 MMSL
4033216 VANDF
703350008 SNOMEDCT_US
11561674 PUBCHEM_CID
CHEBI:78540 CHEBI
CHEMBL514800 ChEMBL_ID
UP7QBP99PN UNII
8872 INN_ID
DB05676 DRUGBANK_ID
7372 IUPHAR_LIGAND_ID
C505730 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Otezla HUMAN PRESCRIPTION DRUG LABEL 1 55513-137 TABLET, FILM COATED 30 mg ORAL NDA 17 sections
Otezla HUMAN PRESCRIPTION DRUG LABEL 3 55513-369 KIT 20 mg None NDA 17 sections
Otezla HUMAN PRESCRIPTION DRUG LABEL 3 55513-369 KIT 10 mg None NDA 17 sections
Otezla HUMAN PRESCRIPTION DRUG LABEL 3 55513-369 KIT 30 mg None NDA 17 sections
Otezla HUMAN PRESCRIPTION DRUG LABEL 3 55513-485 KIT 20 mg None NDA 17 sections
Otezla HUMAN PRESCRIPTION DRUG LABEL 3 55513-485 KIT 30 mg None NDA 17 sections
Otezla HUMAN PRESCRIPTION DRUG LABEL 3 55513-485 KIT 10 mg None NDA 17 sections
OTEZLA HUMAN PRESCRIPTION DRUG LABEL 3 59572-630 KIT 20 mg ORAL NDA 17 sections
OTEZLA HUMAN PRESCRIPTION DRUG LABEL 3 59572-630 KIT 30 mg ORAL NDA 17 sections
OTEZLA HUMAN PRESCRIPTION DRUG LABEL 3 59572-630 KIT 10 mg ORAL NDA 17 sections
OTEZLA HUMAN PRESCRIPTION DRUG LABEL 1 59572-631 TABLET, FILM COATED 30 mg ORAL NDA 17 sections
OTEZLA HUMAN PRESCRIPTION DRUG LABEL 3 59572-632 KIT 20 mg ORAL NDA 17 sections
OTEZLA HUMAN PRESCRIPTION DRUG LABEL 3 59572-632 KIT 10 mg ORAL NDA 17 sections
OTEZLA HUMAN PRESCRIPTION DRUG LABEL 3 59572-632 KIT 30 mg ORAL NDA 17 sections