apremilast Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
60 mg O

ADMET properties:

PropertyValueReference
CL (Clearance) 2.38 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.32 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 6.03 hours Lombardo F, Berellini G, Obach RS

Approvals:

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

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
Diarrhoea 20479.44 68.85 7287 30115 76277 2244406
Nausea 18480.88 68.85 7314 30088 104875 2215808
Psoriasis 17007.27 68.85 4421 32981 12587 2308096
Headache 13793.70 68.85 5435 31967 74744 2245939
Drug ineffective 5676.83 68.85 3199 34203 98425 2222258
Product dose omission 5482.76 68.85 2303 35099 35954 2284729
Abdominal discomfort 5408.29 68.85 1849 35553 15607 2305076
Psoriatic arthropathy 4403.40 68.85 1128 36274 2786 2317897
Depression 3178.01 68.85 1437 35965 26695 2293988
Weight decreased 2725.42 68.85 1296 36106 27075 2293608
Vomiting 2167.55 68.85 1542 35860 70060 2250623
Adverse drug reaction 2112.86 68.85 762 36640 7521 2313162
Abdominal pain upper 2047.55 68.85 986 36416 21114 2299569
Rash 1554.52 68.85 1175 36227 58383 2262300
Therapy non-responder 1353.91 68.85 548 36854 7556 2313127
Migraine 1282.98 68.85 571 36831 10082 2310601
Insomnia 1074.64 68.85 680 36722 25107 2295576
Arthralgia 1017.43 68.85 884 36518 53401 2267282
Decreased appetite 1006.42 68.85 681 36721 28210 2292473
Gastric disorder 965.91 68.85 347 37055 3363 2317320
Pain 939.17 68.85 895 36507 60962 2259721
Frequent bowel movements 921.57 68.85 286 37116 1668 2319015
Dyspepsia 872.36 68.85 427 36975 9417 2311266
Malaise 854.21 68.85 810 36592 54775 2265908
Fatigue 839.71 68.85 977 36425 83896 2236787
Pruritus 801.38 68.85 701 36701 42639 2278044
Upper respiratory tract infection 766.44 68.85 378 37024 8473 2312210
Gastrointestinal disorder 687.38 68.85 352 37050 8565 2312118
Therapeutic product effect decreased 600.07 68.85 343 37059 10446 2310237
Nasopharyngitis 594.13 68.85 445 36957 21611 2299072
Therapeutic response decreased 592.33 68.85 297 37105 6898 2313785
Muscle spasms 573.95 68.85 432 36970 21134 2299549
Stress 558.24 68.85 282 37120 6656 2314027
Dizziness 502.65 68.85 629 36773 58036 2262647
Sinusitis 475.31 68.85 347 37055 16179 2304504
Tension headache 458.68 68.85 125 37277 417 2320266
Alopecia 446.61 68.85 376 37026 21625 2299058
Cough 437.20 68.85 445 36957 32672 2288011
Gastrooesophageal reflux disease 411.04 68.85 253 37149 8842 2311841
Influenza 408.64 68.85 288 37114 12690 2307993
Memory impairment 386.63 68.85 278 37124 12645 2308038
Abdominal pain 370.74 68.85 415 36987 33959 2286724
Flatulence 367.03 68.85 185 37217 4340 2316343
Faeces soft 355.09 68.85 98 37304 347 2320336
Pain in extremity 350.91 68.85 448 36954 42092 2278591
Back pain 334.12 68.85 378 37024 31281 2289402
Unevaluable event 328.87 68.85 218 37184 8673 2312010
Arthropathy 321.60 68.85 200 37202 7116 2313567
Anxiety 290.28 68.85 339 37063 29020 2291663
Bronchitis 285.55 68.85 238 37164 13476 2307207
Peripheral swelling 283.55 68.85 264 37138 17333 2303350
Condition aggravated 265.41 68.85 338 37064 31641 2289042
Therapeutic product effect incomplete 247.12 68.85 196 37206 10335 2310348
Arthritis 245.73 68.85 191 37211 9777 2310906
Feeling abnormal 244.29 68.85 279 37123 23302 2297381
Abdominal distension 236.26 68.85 190 37212 10221 2310462
Rhinorrhoea 223.40 68.85 161 37241 7339 2313344
Mood altered 204.44 68.85 106 37296 2640 2318043
Tremor 186.67 68.85 228 37174 20433 2300250
Enthesopathy 186.56 68.85 48 37354 119 2320564
Discomfort 179.90 68.85 122 37280 5037 2315646
Gastroenteritis viral 174.93 68.85 93 37309 2441 2318242
Urinary tract infection 174.29 68.85 267 37135 29675 2291008
Depressed mood 171.98 68.85 119 37283 5079 2315604
Dry skin 171.64 68.85 131 37271 6521 2314162
Suicidal ideation 168.29 68.85 161 37241 10926 2309757
Myalgia 163.26 68.85 227 37175 23106 2297577
Loss of personal independence in daily activities 160.41 68.85 115 37287 5196 2315487
Treatment failure 159.73 68.85 130 37272 7109 2313574
Nasal congestion 155.60 68.85 126 37276 6840 2313843
Rash pruritic 155.16 68.85 130 37272 7405 2313278
Therapy cessation 153.54 68.85 111 37291 5082 2315601
Musculoskeletal stiffness 153.00 68.85 160 37242 12087 2308596
Skin exfoliation 149.32 68.85 114 37288 5676 2315007
Joint swelling 149.30 68.85 184 37218 16635 2304048
Constipation 146.21 68.85 207 37195 21422 2299261
Drug intolerance 141.44 68.85 162 37240 13555 2307128
Ear infection 128.68 68.85 85 37317 3356 2317327
Hypersensitivity 128.34 68.85 204 37198 23389 2297294
Palpitations 127.07 68.85 168 37234 16288 2304395
Rheumatoid arthritis 117.43 68.85 175 37227 18965 2301718
Multiple allergies 111.84 68.85 49 37353 826 2319857
Sinus headache 110.60 68.85 50 37352 911 2319772
Pregnancy 108.60 68.85 109 37293 7840 2312843
Sinus disorder 104.64 68.85 68 37334 2610 2318073
Skin discolouration 104.38 68.85 90 37312 5330 2315353
Incorrect dose administered 104.17 68.85 117 37285 9578 2311105
Mood swings 103.82 68.85 73 37329 3196 2317487
Synovitis 101.11 68.85 67 37335 2659 2318024
Retching 101.03 68.85 61 37341 2053 2318630
Rebound psoriasis 98.22 68.85 21 37381 12 2320671
Infection 95.42 68.85 154 37248 17875 2302808
Crying 92.88 68.85 77 37325 4319 2316364
Nephrolithiasis 90.67 68.85 77 37325 4466 2316217
Respiratory tract infection 90.22 68.85 73 37329 3956 2316727
Blood pressure increased 89.77 68.85 145 37257 16841 2303842
Tenosynovitis 86.35 68.85 35 37367 481 2320202
Back disorder 83.23 68.85 49 37353 1573 2319110
Defaecation urgency 82.78 68.85 32 37370 385 2320298
Therapy partial responder 80.71 68.85 31 37371 366 2320317
Irritable bowel syndrome 80.01 68.85 50 37352 1791 2318892
Diverticulitis 79.87 68.85 69 37333 4096 2316587
Joint stiffness 77.86 68.85 67 37335 3956 2316727
Irritability 76.74 68.85 82 37320 6345 2314338
Urticaria 75.43 68.85 165 37237 24096 2296587
Rash macular 74.91 68.85 62 37340 3469 2317214
Skin disorder 73.40 68.85 62 37340 3569 2317114
Adverse event 73.15 68.85 87 37315 7572 2313111
Feeling jittery 72.90 68.85 48 37354 1884 2318799
Eructation 72.81 68.85 40 37362 1122 2319561
Oropharyngeal pain 70.17 68.85 105 37297 11413 2309270

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
Diarrhoea 10782.36 88.23 3957 16796 49895 1676133
Psoriasis 9124.44 88.23 2450 18303 9175 1716853
Nausea 6260.54 88.23 2659 18094 48537 1677491
Headache 6028.81 88.23 2319 18434 32057 1693971
Drug ineffective 4105.07 88.23 2136 18617 61665 1664363
Abdominal discomfort 3712.71 88.23 1161 19592 7920 1718108
Product dose omission 3262.26 88.23 1331 19422 21109 1704919
Psoriatic arthropathy 2013.86 88.23 534 20219 1769 1724259
Depression 1663.31 88.23 761 19992 15908 1710120
Weight decreased 1444.01 88.23 763 19990 21990 1704038
Abdominal pain upper 1270.17 88.23 557 20196 10444 1715584
Adverse drug reaction 1165.68 88.23 415 20338 4323 1721705
Therapy non-responder 907.23 88.23 373 20380 5893 1720135
Rash 715.40 88.23 602 20151 38091 1687937
Frequent bowel movements 702.02 88.23 213 20540 1261 1724767
Therapeutic product effect decreased 614.39 88.23 284 20469 6013 1720015
Gastric disorder 575.26 88.23 194 20559 1684 1724344
Arthralgia 554.35 88.23 422 20331 23022 1703006
Fatigue 457.03 88.23 534 20219 50247 1675781
Decreased appetite 441.01 88.23 372 20381 23499 1702529
Therapeutic response decreased 423.62 88.23 211 20542 5289 1720739
Insomnia 419.93 88.23 309 20444 15967 1710061
Gastrointestinal disorder 413.16 88.23 198 20555 4550 1721478
Dyspepsia 400.99 88.23 197 20556 4788 1721240
Vomiting 386.73 88.23 428 20325 37887 1688141
Pain 376.43 88.23 357 20396 26300 1699728
Flatulence 358.39 88.23 155 20598 2779 1723249
Pruritus 356.71 88.23 326 20427 22896 1703132
Memory impairment 355.30 88.23 200 20553 6463 1719565
Faeces soft 354.97 88.23 93 20660 286 1725742
Nasopharyngitis 306.23 88.23 211 20542 9799 1716229
Upper respiratory tract infection 288.64 88.23 148 20605 3945 1722083
Dizziness 274.87 88.23 341 20412 34020 1692008
Mood altered 265.32 88.23 114 20639 2008 1724020
Malaise 243.72 88.23 298 20455 29267 1696761
Migraine 233.74 88.23 107 20646 2204 1723824
Tension headache 230.07 88.23 61 20692 199 1725829
Abdominal pain 217.80 88.23 241 20512 21249 1704779
Enthesopathy 187.20 88.23 43 20710 59 1725969
Muscle spasms 179.71 88.23 164 20589 11457 1714571
Anxiety 178.09 88.23 186 20567 15341 1710687
Unevaluable event 176.31 88.23 124 20629 5942 1720086
Feeling abnormal 169.58 88.23 156 20597 11010 1715018
Back pain 164.23 88.23 184 20569 16429 1709599
Treatment failure 161.54 88.23 104 20649 4297 1721731
Arthritis 161.06 88.23 100 20653 3875 1722153
Sinusitis 159.34 88.23 110 20643 5113 1720915
Influenza 157.53 88.23 121 20632 6646 1719382
Arthropathy 149.81 88.23 85 20668 2782 1723246
Rhinorrhoea 147.31 88.23 94 20659 3823 1722205
Discomfort 145.46 88.23 81 20672 2555 1723473
Cough 144.35 88.23 185 20568 19012 1707016
Suicidal ideation 143.10 88.23 126 20627 8392 1717636
Tenosynovitis 137.50 88.23 42 20711 254 1725774
C-reactive protein abnormal 137.42 88.23 41 20712 226 1725802
Loss of personal independence in daily activities 130.42 88.23 73 20680 2326 1723702
Therapeutic product effect incomplete 125.87 88.23 97 20656 5351 1720677
Depressed mood 125.03 88.23 77 20676 2939 1723089
Peripheral swelling 124.16 88.23 113 20640 7858 1718170
Mood swings 120.06 88.23 65 20688 1937 1724091
Drug intolerance 114.67 88.23 96 20657 5966 1720062
Abdominal distension 111.58 88.23 97 20656 6347 1719681
Pain in extremity 109.98 88.23 159 20594 18313 1707715
Gastrooesophageal reflux disease 107.92 88.23 83 20670 4564 1721464
Synovitis 106.36 88.23 44 20709 701 1725327
Stress 103.33 88.23 65 20688 2576 1723452
Skin exfoliation 94.52 88.23 76 20677 4459 1721569
Dry skin 92.15 88.23 69 20684 3643 1722385

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