progesterone Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
steroids, progestogens 2279 57-83-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • progesterone
  • gestone
  • gestormone
  • glanducorpin
  • lugesteron
  • lugesterone
  • progestan
  • progeston
  • progestone
  • progestron
  • progesterol
  • syngesterone
The major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production. Progesterone, converted from PREGNENOLONE, also serves as an intermediate in the biosynthesis of GONADAL STEROID HORMONES and adrenal CORTICOSTEROIDS.
  • Molecular weight: 314.47
  • Formula: C21H30O2
  • CLOGP: 3.96
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 34.14
  • ALOGS: -4.76
  • ROTB: 1

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.30 g O
5 mg P
0.20 g R
90 mg V

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.01 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) 21.20 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 25 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Feb. 4, 1976 FDA ALZA

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
Ovarian hyperstimulation syndrome 326.52 39.25 52 829 666 2356538
Maternal exposure during pregnancy 254.26 39.25 71 810 14792 2342412
Temperature regulation disorder 224.57 39.25 31 850 130 2357074
Food allergy 196.11 39.25 33 848 598 2356606
Coeliac disease 173.69 39.25 31 850 801 2356403
Exposure during pregnancy 173.26 39.25 60 821 25159 2332045
Immunodeficiency 165.73 39.25 31 850 1045 2356159
Hypersensitivity 149.86 39.25 53 828 23540 2333664
Bursitis 148.02 39.25 31 850 1877 2355327
Drug hypersensitivity 134.12 39.25 59 822 46584 2310620
Abortion spontaneous 123.83 39.25 40 841 13405 2343799
Rash erythematous 122.19 39.25 33 848 5943 2351261
Meningioma 121.04 39.25 22 859 628 2356576
Headache 120.44 39.25 65 816 80114 2277090
Hepatic enzyme increased 114.54 39.25 35 846 9767 2347437
Foetal exposure during pregnancy 112.03 39.25 30 851 5222 2351982
Premature labour 111.46 39.25 25 856 2081 2355123
Fluid retention 107.77 39.25 31 850 7015 2350189
Hyperhidrosis 106.67 39.25 37 844 15385 2341819
Upper respiratory tract infection 96.55 39.25 30 851 8821 2348383
Asthma 93.30 39.25 31 850 11283 2345921
Rheumatoid arthritis 91.58 39.25 35 846 19105 2338099
Human herpesvirus 6 infection 91.46 39.25 16 865 364 2356840
Constipation 90.93 39.25 36 845 21593 2335611
Erythema 89.04 39.25 37 844 25122 2332082
Fatigue 82.44 39.25 52 829 84821 2272383
Dizziness 77.84 39.25 44 837 58621 2298583
Vaginal haemorrhage 72.01 39.25 21 860 4959 2352245
Butterfly rash 71.89 39.25 12 869 204 2357000
Premature baby 71.54 39.25 19 862 3185 2354019
Pain 70.37 39.25 42 839 61815 2295389
Back pain 68.44 39.25 33 848 31626 2325578
Multiple-drug resistance 63.74 39.25 11 870 230 2356974
Ectopic pregnancy 62.47 39.25 13 868 755 2356449
Premature delivery 62.14 39.25 17 864 3183 2354021
Product use issue 60.77 39.25 23 858 12146 2345058
Gestational diabetes 60.07 39.25 14 867 1373 2355831
Off label use 58.80 39.25 40 841 73558 2283646
Ascites 56.81 39.25 18 863 5602 2351602
Suicidal behaviour 55.27 39.25 11 870 510 2356694
Periorbital oedema 53.33 39.25 12 869 1006 2356198
Head discomfort 52.56 39.25 13 868 1638 2355566
Hot flush 52.43 39.25 18 863 7181 2350023
Ophthalmic vein thrombosis 51.96 39.25 7 874 23 2357181
Product use in unapproved indication 51.71 39.25 20 861 11180 2346024
Breast cancer 51.22 39.25 19 862 9476 2347728
Abdominal pain lower 49.67 39.25 14 867 2919 2354285
Cellulitis 48.12 39.25 18 863 9183 2348021
Photosensitivity reaction 47.59 39.25 13 868 2414 2354790
Congenital umbilical hernia 47.23 39.25 7 874 52 2357152
Product odour abnormal 46.27 39.25 9 872 370 2356834
Foetal death 45.81 39.25 12 869 1900 2355304
Pulmonary embolism 45.59 39.25 21 860 18062 2339142
Contraindicated product administered 44.78 39.25 13 868 3008 2354196
Vaginal discharge 43.36 39.25 10 871 935 2356269
Drug ineffective 41.17 39.25 37 844 101587 2255617
Caesarean section 40.92 39.25 13 868 4068 2353136
Ovarian cyst 40.70 39.25 11 870 1962 2355242
Rash 39.60 39.25 29 852 59529 2297675

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
Foetal exposure during pregnancy 315.84 171.64 50 31 6309 1740391

Pharmacologic Action:

SourceCodeDescription
ATC G03DA04 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
PROGESTOGENS
Pregnen (4) derivatives
ATC G03FA04 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
PROGESTOGENS AND ESTROGENS IN COMBINATION
Progestogens and estrogens, fixed combinations
FDA Chemical/Ingredient N0000005934 Progesterone
CHEBI has role CHEBI:49323 contraceptive drug
CHEBI has role CHEBI:70709 progesterone receptor agonist
MeSH PA D006728 Hormones
MeSH PA D011372 Progestins

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Contraception indication 13197004
Dysfunctional uterine bleeding indication 19155002
Atrophic vaginitis indication 52441000
Secondary physiologic amenorrhea indication 86030004
Secondary malignant neoplasm of kidney indication 94360002
Postmenopausal osteoporosis indication 102447009
Endometriosis indication 129103003
Menopausal flushing indication 198436008
Endometrial carcinoma indication 254878006 DOID:2871
Infertility Secondary to Progesterone Deficiency indication
Amenorrhea Secondary to Ovarian Dysfunction indication
Prevention of Premature Labor indication
Endometrial Hyperplasia Prevention indication
Corpus Luteum Insufficiency Syndrome indication
Polycystic ovaries off-label use 69878008
Menorrhagia off-label use 386692008
Precocious puberty off-label use 400179000
Endogenous Estrogen Production Test off-label use
Female Hormonal Imbalance off-label use
Hyperlipoproteinemia contraindication 3744001 DOID:1168
Hypocalcemia contraindication 5291005
Alcoholism contraindication 7200002
Weight gain finding contraindication 8943002
Impaired glucose tolerance contraindication 9414007
Hypercholesterolemia contraindication 13644009
Jaundice contraindication 18165001
Myocardial infarction contraindication 22298006 DOID:5844
Fibroadenosis of breast contraindication 23260002 DOID:10352
Diplopia contraindication 24982008
Retinal hemorrhage contraindication 28998008
Ectopic pregnancy contraindication 34801009 DOID:0060329
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
Mild pre-eclampsia contraindication 41114007
Body fluid retention contraindication 43498006
Thrombosis of retinal vein contraindication 46085004
Humoral hypercalcemia of malignancy contraindication 47709007
Chronic heart failure contraindication 48447003
Dementia contraindication 52448006
Hepatic porphyria contraindication 55056006 DOID:3133
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Hyperlipidemia contraindication 55822004 DOID:1168
Anorexia nervosa contraindication 56882008 DOID:8689
Hepatic failure contraindication 59927004
Cerebrovascular disease contraindication 62914000 DOID:6713
Thrombophlebitis contraindication 64156001 DOID:3875
Osteoporosis contraindication 64859006 DOID:11476
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
Kidney disease contraindication 90708001 DOID:557
Malignant neoplasm of liver contraindication 93870000 DOID:3571
Uterine leiomyoma contraindication 95315005 DOID:13223
Neoplasm of liver contraindication 126851005 DOID:3571
Deep venous thrombosis contraindication 128053003
Seizure disorder contraindication 128613002
Incomplete miscarriage contraindication 156072005
Bed-ridden contraindication 160685001
Mammography abnormal contraindication 168750009
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
Chorea contraindication 271700006
Pregnancy, function contraindication 289908002
Hypertriglyceridemia contraindication 302870006
Osteopenia contraindication 312894000
Functional visual loss contraindication 313165001
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
Optic disc edema contraindication 423341008 DOID:146
Family history of malignant neoplasm of breast contraindication 429740004
Hypertensive urgency contraindication 443482000
Carcinoma of female breast contraindication 447782002
Smokes tobacco daily contraindication 449868002
Predisposition to Thrombosis contraindication

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
100MG BIJUVA THERAPEUTICSMD INC N210132 Oct. 28, 2018 RX CAPSULE ORAL 10206932 Nov. 21, 2032 TREATMENT OF MENOPAUSE SYMPTOMS, INCLUDING VASOMOTOR SYMPTOMS
100MG BIJUVA THERAPEUTICSMD INC N210132 Oct. 28, 2018 RX CAPSULE ORAL 8846648 Nov. 21, 2032 TREATMENT OF MENOPAUSE SYMPTOMS, INCLUDING VASOMOTOR SYMPTOMS
100MG BIJUVA THERAPEUTICSMD INC N210132 Oct. 28, 2018 RX CAPSULE ORAL 8846649 Nov. 21, 2032 TREATMENT OF MENOPAUSE SYMPTOMS, INCLUDING VASOMOTOR SYMPTOMS
100MG BIJUVA THERAPEUTICSMD INC N210132 Oct. 28, 2018 RX CAPSULE ORAL 9006222 Nov. 21, 2032 TREATMENT OF MENOPAUSE SYMPTOMS, INCLUDING VASOMOTOR SYMPTOMS
100MG BIJUVA THERAPEUTICSMD INC N210132 Oct. 28, 2018 RX CAPSULE ORAL 9114145 Nov. 21, 2032 TREATMENT OF MENOPAUSE SYMPTOMS, INCLUDING VASOMOTOR SYMPTOMS
100MG BIJUVA THERAPEUTICSMD INC N210132 Oct. 28, 2018 RX CAPSULE ORAL 9114146 Nov. 21, 2032 TREATMENT OF MENOPAUSE SYMPTOMS, INCLUDING VASOMOTOR SYMPTOMS
100MG BIJUVA THERAPEUTICSMD INC N210132 Oct. 28, 2018 RX CAPSULE ORAL 9301920 Nov. 21, 2032 TREATMENT OF MENOPAUSE SYMPTOMS, INCLUDING VASOMOTOR SYMPTOMS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG BIJUVA THERAPEUTICSMD INC N210132 Oct. 28, 2018 RX CAPSULE ORAL Oct. 28, 2021 NEW PRODUCT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Progesterone receptor Nuclear hormone receptor AGONIST ED50 9.88 WOMBAT-PK CHEMBL
Sodium/nucleoside cotransporter 1 Transporter Ki 5.17 DRUG MATRIX
Sex hormone-binding globulin Secreted Kd 6.94 CHEMBL
Multidrug resistance protein 1 Transporter IC50 4.32 CHEMBL
Glucocorticoid receptor Nuclear hormone receptor Ki 7.52 CHEMBL
Sterol O-acyltransferase 1 Enzyme IC50 4.77 CHEMBL
Androgen receptor Nuclear hormone receptor Ki 8.07 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.59 CHEMBL
Fatty acid-binding protein, intestinal Cytosolic other Ki 4.70 CHEMBL
Mineralocorticoid receptor Nuclear hormone receptor EC50 11 WOMBAT-PK
Estrogen receptor Nuclear hormone receptor WOMBAT-PK
Short transient receptor potential channel 5 Ion channel BLOCKER IC50 5.30 IUPHAR
Cation channel sperm-associated protein 1 Ion channel ACTIVATOR EC50 8.11 IUPHAR
Cation channel sperm-associated protein 4 Ion channel ACTIVATOR EC50 8.11 IUPHAR
Cation channel sperm-associated protein 2 Ion channel ACTIVATOR EC50 8.11 IUPHAR
Cation channel sperm-associated protein 3 Ion channel ACTIVATOR EC50 8.11 IUPHAR
Corticosteroid-binding globulin Secreted Ki 7.38 CHEMBL
Progesterone receptor Transcription factor Ki 8.44 DRUG MATRIX
Progesterone receptor Transcription factor Ki 7.98 CHEMBL
Fatty acid-binding protein, liver Unclassified Ki 7.57 CHEMBL
Androgen receptor Transcription factor IC50 7.43 CHEMBL
Estrogen receptor Transcription factor Kd 8.41 CHEMBL
Androgen receptor Transcription factor IC50 5.81 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Kd 6.62 CHEMBL
Steroid 5-alpha-reductase Enzyme IC50 5.80 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane other Ki 6.18 CHEMBL
C-8 sterol isomerase Enzyme Ki 5.35 CHEMBL

External reference:

IDSource
4017453 VUID
N0000145841 NUI
C0033308 UMLSCUI
D00066 KEGG_DRUG
4G7DS2Q64Y UNII
417 INN_ID
50318003 SNOMEDCT_US
4017453 VANDF
2110 MMSL
8727 RXNORM
16683002 SNOMEDCT_US
5365 MMSL
d00550 MMSL
001290 NDDF
CHEMBL103 ChEMBL_ID
DB00396 DRUGBANK_ID
STR PDB_CHEM_ID
CHEBI:17026 CHEBI
5994 PUBCHEM_CID
D011374 MESH_DESCRIPTOR_UI
C003549 MESH_SUPPLEMENTAL_RECORD_UI
2377 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Crinone HUMAN PRESCRIPTION DRUG LABEL 1 0023-6150 GEL 45 mg VAGINAL NDA 13 sections
Crinone HUMAN PRESCRIPTION DRUG LABEL 1 0023-6151 GEL 90 mg VAGINAL NDA 13 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 0093-5353 CAPSULE, LIQUID FILLED 100 mg ORAL ANDA 14 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 0093-5354 CAPSULE, LIQUID FILLED 200 mg ORAL ANDA 14 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 0143-9725 INJECTION 50 mg INTRAMUSCULAR ANDA 11 sections
PROGESTERONE HUMAN PRESCRIPTION DRUG LABEL 1 0591-3128 INJECTION, SOLUTION 50 mg INTRAMUSCULAR NDA 11 sections
PROGESTERONE HUMAN PRESCRIPTION DRUG LABEL 1 10888-7135 CAPSULE 100 mg ORAL ANDA 13 sections
PROGESTERONE HUMAN PRESCRIPTION DRUG LABEL 1 10888-7136 CAPSULE 200 mg ORAL ANDA 13 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 17478-766 CAPSULE 100 mg ORAL ANDA 15 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 17478-767 CAPSULE 200 mg ORAL ANDA 15 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 43598-349 CAPSULE 100 mg ORAL ANDA 14 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 43598-350 CAPSULE 200 mg ORAL ANDA 14 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 50090-3240 CAPSULE 100 mg ORAL NDA 15 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 50090-4656 CAPSULE 100 mg ORAL ANDA 14 sections
Bijuva HUMAN PRESCRIPTION DRUG LABEL 2 50261-211 CAPSULE 100 mg ORAL NDA 19 sections
Crinone HUMAN PRESCRIPTION DRUG LABEL 1 52544-255 GEL 45 mg VAGINAL NDA 13 sections
Crinone HUMAN PRESCRIPTION DRUG LABEL 1 52544-256 GEL 90 mg VAGINAL NDA 13 sections
Crinone HUMAN PRESCRIPTION DRUG LABEL 1 52544-283 GEL 45 mg VAGINAL NDA 13 sections
Crinone HUMAN PRESCRIPTION DRUG LABEL 1 52544-284 GEL 90 mg VAGINAL NDA 13 sections
Prometrium HUMAN PRESCRIPTION DRUG LABEL 1 54868-4230 CAPSULE 200 mg ORAL NDA 14 sections
Prometrium HUMAN PRESCRIPTION DRUG LABEL 1 54868-4250 CAPSULE 100 mg ORAL NDA 14 sections
Prochieve HUMAN PRESCRIPTION DRUG LABEL 1 55056-0406 GEL 45 mg VAGINAL NDA 14 sections
Crinone HUMAN PRESCRIPTION DRUG LABEL 1 55056-0806 GEL 90 mg VAGINAL NDA 14 sections
Crinone HUMAN PRESCRIPTION DRUG LABEL 1 55056-0808 GEL 45 mg VAGINAL NDA 14 sections
Crinone HUMAN PRESCRIPTION DRUG LABEL 1 55056-0818 GEL 90 mg VAGINAL NDA 14 sections
Prochieve HUMAN PRESCRIPTION DRUG LABEL 1 55056-1601 GEL 90 mg VAGINAL NDA 14 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 55150-306 INJECTION, SOLUTION 50 mg INTRAMUSCULAR ANDA 11 sections
ENDOMETRIN HUMAN PRESCRIPTION DRUG LABEL 1 55566-6500 INSERT 100 mg VAGINAL NDA 17 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 59651-152 CAPSULE 100 mg ORAL ANDA 13 sections
Progesterone HUMAN PRESCRIPTION DRUG LABEL 1 59651-153 CAPSULE 200 mg ORAL ANDA 13 sections