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

Stem definitionDrug idCAS RN
steroids, progestogens 818 54024-22-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • Org 2969
  • desogestrel
  • cerazette
A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents (ORAL CONTRACEPTIVES, COMBINED).
  • Molecular weight: 310.48
  • Formula: C22H30O
  • CLOGP: 5.50
  • LIPINSKI: 1
  • HAC: 1
  • HDO: 1
  • TPSA: 20.23
  • ALOGS: -5.01
  • ROTB: 1
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.32 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.01 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 5 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Dec. 10, 1992 FDA ORGANON USA INC

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
Pregnancy on oral contraceptive 75.18 19.81 19 8233 1018 63479752
Muscle injury 56.37 19.81 55 8197 65290 63415480
Folliculitis 54.79 19.81 56 8196 70261 63410509
Irritable bowel syndrome 54.24 19.81 60 8192 82352 63398418
Lower respiratory tract infection 47.05 19.81 71 8181 132236 63348534
Blister 42.42 19.81 67 8185 129747 63351023
Impaired healing 40.74 19.81 58 8194 102484 63378286
Meningioma 39.81 19.81 16 8236 3869 63476901
Hepatocellular injury 39.71 19.81 31 8221 27350 63453420
Gastrointestinal disorder 36.50 19.81 63 8189 131176 63349594
Lip swelling 36.27 19.81 31 8221 31032 63449738
Peripheral swelling 34.82 19.81 94 8158 265848 63214922
Night sweats 34.64 19.81 37 8215 48777 63431993
Stomatitis 32.72 19.81 62 8190 138663 63342107
Peripheral venous disease 30.29 19.81 21 8231 15456 63465314
Pruritus 29.11 19.81 108 8144 361345 63119425
Essential tremor 28.53 19.81 9 8243 1079 63479691
Polymenorrhagia 27.76 19.81 5 8247 50 63480720
Facet joint syndrome 27.41 19.81 18 8234 12120 63468650
Labelled drug-food interaction medication error 27.18 19.81 6 8246 178 63480592
Hyperprolactinaemia 26.49 19.81 12 8240 3888 63476882
Maculopathy 25.57 19.81 10 8242 2252 63478518
Vaginal haemorrhage 25.31 19.81 24 8228 27463 63453307
Pneumonia 25.27 19.81 14 8238 456753 63024017
Urticaria 25.17 19.81 62 8190 165740 63315030
Lip dry 23.48 19.81 18 8234 15452 63465318
Sleep disorder due to general medical condition, insomnia type 22.91 19.81 31 8221 52186 63428584
Personality change 22.54 19.81 13 8239 6960 63473810
Swollen tongue 22.29 19.81 25 8227 34775 63445995
XIth nerve injury 21.54 19.81 4 8248 48 63480722
Exposure keratitis 21.47 19.81 4 8248 49 63480721
Tracheal pain 21.39 19.81 4 8248 50 63480720
Weight increased 21.02 19.81 78 8174 260714 63220056
Meningioma surgery 20.90 19.81 4 8248 57 63480713
Cell death 20.88 19.81 9 8243 2592 63478178
Hypersensitivity 20.71 19.81 84 8168 292601 63188169
Reversible cerebral vasoconstriction syndrome 20.69 19.81 9 8243 2649 63478121
Fall 20.31 19.81 13 8239 392321 63088449
Joint range of motion decreased 20.27 19.81 23 8229 32405 63448365
Nasal mucosal erosion 20.13 19.81 4 8248 70 63480700
Helicobacter infection 20.07 19.81 40 8212 92745 63388025
Obesity 20.01 19.81 22 8230 29930 63450840

FDA Adverse Event Reporting System (Male)

None

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
Pregnancy on oral contraceptive 80.75 22.83 18 7059 827 79736484
Muscle injury 60.33 22.83 43 7034 48518 79688793
Irritable bowel syndrome 57.14 22.83 46 7031 62195 79675116
Folliculitis 53.12 22.83 42 7035 55338 79681973
Blister 44.64 22.83 54 7023 119422 79617889
Lower respiratory tract infection 44.41 22.83 56 7021 129164 79608147
Lip swelling 39.17 22.83 31 7046 40880 79696431
Night sweats 38.52 22.83 34 7043 52061 79685250
Impaired healing 38.39 22.83 43 7034 87612 79649699
Peripheral venous disease 37.13 22.83 21 7056 15888 79721423
Gastrointestinal disorder 35.85 22.83 49 7028 122156 79615155
Hepatocellular injury 35.07 22.83 31 7046 47562 79689749
Facet joint syndrome 35.00 22.83 18 7059 11284 79726027
Peripheral swelling 34.80 22.83 75 7002 269542 79467769
Helicobacter infection 33.65 22.83 36 7041 69668 79667643
Vaginal haemorrhage 33.43 22.83 22 7055 21795 79715516
Urticaria 32.97 22.83 59 7018 185142 79552169
Pruritus 31.14 22.83 91 6986 394557 79342754
Duodenal ulcer perforation 29.87 22.83 33 7044 66178 79671133
Labelled drug-food interaction medication error 29.86 22.83 6 7071 166 79737145
Lip dry 29.77 22.83 18 7059 15400 79721911
Polymenorrhagia 29.76 22.83 5 7072 49 79737262
Sleep disorder due to general medical condition, insomnia type 29.39 22.83 27 7050 43529 79693782
Pericarditis 29.37 22.83 41 7036 104195 79633116
Maternal exposure during pregnancy 28.91 22.83 47 7030 136491 79600820
Essential tremor 28.74 22.83 9 7068 1546 79735765
Stomatitis 27.72 22.83 48 7029 146709 79590602
Pneumonia 27.72 22.83 12 7065 660234 79077077
Maculopathy 27.12 22.83 10 7067 2815 79734496
Meningioma 26.37 22.83 11 7066 4287 79733024
Hypersensitivity 26.20 22.83 66 7011 262173 79475138
Joint range of motion decreased 25.16 22.83 22 7055 33260 79704051
Swollen tongue 24.18 22.83 24 7053 42546 79694765
Obesity 24.13 22.83 22 7055 35103 79702208
Rash 23.90 22.83 108 6969 578250 79159061
Pemphigus 23.45 22.83 36 7041 99546 79637765
Systemic lupus erythematosus 23.37 22.83 40 7037 121109 79616202
Swelling 23.18 22.83 56 7021 216655 79520656

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC G03AA09 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE
Progestogens and estrogens, fixed combinations
ATC G03AB05 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE
Progestogens and estrogens, sequential preparations
ATC G03AC09 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE
Progestogens
ATC G03FB10 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
PROGESTOGENS AND ESTROGENS IN COMBINATION
Progestogens and estrogens, sequential preparations
FDA CS M0447349 Progesterone Congeners
CHEBI has role CHEBI:49323 contraceptive drugs
CHEBI has role CHEBI:49326 synthetic oral contraceptives
CHEBI has role CHEBI:59826 progestins
FDA EPC N0000175602 Progestin
MeSH PA D003270 Contraceptive Agents
MeSH PA D003271 Contraceptive Agents, Female
MeSH PA D000080066 Contraceptive Agents, Hormonal
MeSH PA D003278 Contraceptives, Oral, Hormonal
MeSH PA D003280 Contraceptives, Oral, Synthetic
MeSH PA D006728 Hormones
MeSH PA D011372 Progestins
MeSH PA D012102 Reproductive Control Agents

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

DiseaseRelationSNOMED_IDDOID
Contraception indication 13197004
Amenorrhea off-label use 14302001 DOID:13938
Female hypogonadism syndrome off-label use 16041008
Polycystic ovaries off-label use 69878008
Dysmenorrhea off-label use 266599000
Abnormal uterine bleeding unrelated to menstrual cycle off-label use 312984006
Menorrhagia off-label use 386692008
Heart valve disorder contraindication 368009 DOID:4079
Hyperlipoproteinemia contraindication 3744001 DOID:1168
Hypocalcemia contraindication 5291005
Hypercholesterolemia contraindication 13644009
Myocardial infarction contraindication 22298006 DOID:5844
Depressive disorder contraindication 35489007
Chloasma contraindication 36209000
Migraine contraindication 37796009 DOID:6364
Hypertensive disorder contraindication 38341003 DOID:10763
Disorder of gallbladder contraindication 39621005 DOID:0060262
Hypothyroidism contraindication 40930008 DOID:1459
Body fluid retention contraindication 43498006
Thrombosis of retinal vein contraindication 46085004
Humoral hypercalcemia of malignancy contraindication 47709007
Dementia contraindication 52448006
Hepatic porphyria contraindication 55056006 DOID:3133
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Hyperlipidemia contraindication 55822004 DOID:1168
Benign mammary dysplasia contraindication 57993004
Obstructive hyperbilirubinemia contraindication 59848001
Thrombophlebitis contraindication 64156001 DOID:3875
Intermenstrual bleeding - irregular contraindication 64996003
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Epilepsy contraindication 84757009 DOID:1826
Breast lump contraindication 89164003
Malignant neoplasm of liver contraindication 93870000 DOID:3571
Uterine leiomyoma contraindication 95315005 DOID:13223
Deep venous thrombosis contraindication 128053003
Endometriosis contraindication 129103003
Liver function tests abnormal contraindication 166603001
Mammography abnormal contraindication 168750009
Angina pectoris contraindication 194828000
Asthma contraindication 195967001 DOID:2841
Cerebrovascular accident contraindication 230690007
Pulmonary thromboembolism contraindication 233935004
Thrombophilia contraindication 234467004 DOID:2452
Disease of liver contraindication 235856003 DOID:409
Cholestasis of pregnancy contraindication 235888006
Endometrial carcinoma contraindication 254878006 DOID:2871
Chorea contraindication 271700006
Pregnancy, function contraindication 289908002
Hypertriglyceridemia contraindication 302870006
Functional visual loss contraindication 313165001
Malignant tumor of cervix contraindication 363354003 DOID:4362
Malignant tumor of ovary contraindication 363443007 DOID:2394
Thromboembolic disorder contraindication 371039008
Cardiovascular event risk contraindication 395112001
Disorder of coronary artery contraindication 414024009
Obesity contraindication 414916001 DOID:9970
Estrogen receptor positive tumor contraindication 416053008
Porphyria contraindication 418470004
Family history of malignant neoplasm of breast contraindication 429740004
Hypertensive urgency contraindication 443482000
Carcinoma of female breast contraindication 447782002
Smokes tobacco daily contraindication 449868002
Nonspecific Abnormal Papanicolaou Smear of Cervix contraindication
Major Surgery with Prolonged Post-Operative Immobilization contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.93 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Progesterone receptor Nuclear hormone receptor AGONIST WOMBAT-PK CHEMBL
Sex hormone-binding globulin Secreted Kd 6.60 CHEMBL

External reference:

IDSource
4020568 VUID
N0000148270 NUI
D02367 KEGG_DRUG
22656 RXNORM
4020568 VANDF
C0057558 UMLSCUI
CHEBI:4453 CHEBI
CHEMBL1533 ChEMBL_ID
DB00304 DRUGBANK_ID
D017135 MESH_DESCRIPTOR_UI
40973 PUBCHEM_CID
7065 IUPHAR_LIGAND_ID
4384 INN_ID
81K9V7M3A3 UNII
4549 MMSL
d03780 MMSL
003956 NDDF
116074007 SNOMEDCT_US
126108008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
MERCILON HUMAN OTC DRUG LABEL 2 72689-0020 TABLET 0.15 mg ORAL unapproved drug other 7 sections