megestrol acetate ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
steroids, progestogens 1667 595-33-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • megestrol acetate
  • magestin
  • megestryl acetate
  • niagestin
Megestrol acetate is a progestogen with actions and uses similar to those of the progestogens in general. It also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia. (From Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995)
  • Molecular weight: 384.52
  • Formula: C24H32O4
  • CLOGP: 3.77
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 60.44
  • ALOGS: -5.06
  • ROTB: 3

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
5 mg O
0.16 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 60 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 23.22 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 90 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Aug. 18, 1971 FDA BRISTOL MYERS SQUIBB

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
Death 109.50 20.36 147 5170 341279 55945471
Decreased appetite 107.20 20.36 117 5200 219114 56067636
Malignant neoplasm progression 70.13 20.36 57 5260 73530 56213220
Neutropenia 64.57 20.36 77 5240 158090 56128660
Disease progression 59.89 20.36 61 5256 105112 56181638
Deep vein thrombosis 53.85 20.36 50 5267 76927 56209823
Metastases to liver 52.78 20.36 30 5287 21556 56265194
Dehydration 50.04 20.36 68 5249 158757 56127993
Asthenia 41.07 20.36 96 5221 342877 55943873
Breast cancer metastatic 39.16 20.36 22 5295 15447 56271303
Metastases to bone 36.94 20.36 23 5294 19485 56267265
Diarrhoea 33.00 20.36 133 5184 638374 55648376
Oestrogen receptor assay positive 28.41 20.36 7 5310 467 56286283
Meningioma 27.44 20.36 11 5306 3643 56283107
Rheumatoid arthritis 25.78 20.36 3 5314 382601 55904149
Papillary thyroid cancer 25.44 20.36 9 5308 2115 56284635
Breast cancer 23.62 20.36 26 5291 48807 56237943
Abdominal pain 23.17 20.36 65 5252 258740 56028010
Weight decreased 23.08 20.36 62 5255 240652 56046098
Hypoaesthesia oral 22.97 20.36 14 5303 11417 56275333
Thoracic vertebral fracture 22.53 20.36 10 5307 4253 56282497
Dysgeusia 21.92 20.36 23 5294 40892 56245858
Gastritis 21.31 20.36 21 5296 34681 56252069
Pulmonary embolism 21.16 20.36 37 5280 107087 56179663
Anaemia 20.89 20.36 64 5253 267447 56019303

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
Decreased appetite 80.26 19.68 122 6056 153095 31538071
Death 76.61 19.68 196 5982 360373 31330793
Malignant neoplasm progression 76.01 19.68 85 6093 78913 31612253
Asthenia 66.05 19.68 139 6039 224616 31466550
Dehydration 63.92 19.68 96 6082 119015 31572151
Adrenal insufficiency 60.38 19.68 35 6143 12624 31678542
Respiratory tract infection bacterial 56.89 19.68 18 6160 1448 31689718
Pneumonia 52.11 19.68 163 6015 335149 31356017
Respiratory tract infection viral 51.28 19.68 18 6160 1996 31689170
Fatigue 44.03 19.68 154 6024 335052 31356114
Disease progression 41.62 19.68 68 6110 90396 31600770
Pulmonary embolism 39.78 19.68 63 6115 81583 31609583
Anaemia 30.45 19.68 101 6077 213421 31477745
Diarrhoea 28.80 19.68 140 6038 352269 31338897
Respiratory tract infection 24.27 19.68 23 6155 17538 31673628
Dysphagia 23.37 19.68 41 6137 57635 31633531
Weight decreased 22.17 19.68 75 6103 159877 31531289
Drug ineffective 21.98 19.68 27 6151 395546 31295620
Plasma cell myeloma 20.12 19.68 38 6140 56493 31634673

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
Decreased appetite 128.36 18.85 170 8371 304610 70615293
Death 124.91 18.85 221 8320 509840 70410063
Dehydration 99.49 18.85 129 8412 226013 70693890
Adrenal insufficiency 76.80 18.85 44 8497 25151 70894752
Asthenia 70.66 18.85 164 8377 457502 70462401
Malignant neoplasm progression 68.97 18.85 79 8462 121660 70798243
Respiratory tract infection bacterial 62.42 18.85 18 8523 1719 70918184
Pulmonary embolism 59.40 18.85 83 8458 155784 70764119
Disease progression 59.07 18.85 83 8458 156589 70763314
Pneumonia 57.93 18.85 180 8361 596052 70323851
Respiratory tract infection viral 49.81 18.85 18 8523 3523 70916380
Anaemia 43.99 18.85 127 8414 403296 70516607
Diarrhoea 40.08 18.85 193 8348 783148 70136755
Neutropenia 38.27 18.85 91 8450 257065 70662838
Plasma cell myeloma 35.63 18.85 44 8497 73157 70846746
Deep vein thrombosis 33.45 18.85 53 8488 110989 70808914
Fatigue 31.16 18.85 187 8354 824132 70095771
Drug ineffective 28.85 18.85 43 8498 939709 69980194
Platelet count decreased 26.41 18.85 63 8478 178159 70741744
Failure to thrive 25.43 18.85 16 8525 10813 70909090
Constipation 25.09 18.85 77 8464 252361 70667542
Androgen deficiency 24.82 18.85 5 8536 102 70919801
Rheumatoid arthritis 24.82 18.85 3 8538 291802 70628101
Mental status changes 24.59 18.85 34 8507 63067 70856836
Pleural effusion 24.20 18.85 51 8490 132813 70787090
Meningioma 23.85 18.85 11 8530 4007 70915896
Thrombocytopenia 23.82 18.85 73 8468 239037 70680866
Blood testosterone decreased 22.56 18.85 9 8532 2304 70917599
Cachexia 21.69 18.85 14 8527 9886 70910017
Respiratory tract infection 21.45 18.85 26 8515 42372 70877531
Secondary adrenocortical insufficiency 21.39 18.85 9 8532 2638 70917265
Hypophagia 20.24 18.85 25 8516 41545 70878358

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC G03AA04 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 G03AB01 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 G03AC05 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE
Progestogens
ATC G03DB02 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
PROGESTOGENS
Pregnadien derivatives
ATC G03FA08 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
PROGESTOGENS AND ESTROGENS IN COMBINATION
Progestogens and estrogens, fixed combinations
ATC G03FB04 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
PROGESTOGENS AND ESTROGENS IN COMBINATION
Progestogens and estrogens, sequential preparations
ATC L02AB01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONES AND RELATED AGENTS
Progestogens
FDA CS M0447349 Progesterone Congeners
FDA EPC N0000175602 Progestin
MeSH PA D000970 Antineoplastic Agents
MeSH PA D018931 Antineoplastic Agents, Hormonal
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 D012102 Reproductive Control Agents
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:49323 contraceptive drugs
CHEBI has role CHEBI:49326 synthetic oral contraceptives
CHEBI has role CHEBI:50779 appetite enhancing drug
CHEBI has role CHEBI:59826 progestins
MeSH PA D019167 Appetite Stimulants
MeSH PA D002491 Central Nervous System Agents
MeSH PA D000697 Central Nervous System Stimulants

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

DiseaseRelationSNOMED_IDDOID
Endometrial carcinoma indication 254878006 DOID:2871
Hormone receptor positive malignant neoplasm of breast indication 417181009
Nutritional deficiency associated with AIDS indication 420691000
Cachexia due to HIV indication
Anorexia from HIV indication
Malignant tumor of ovary off-label use 363443007 DOID:2394
Hypertensive disorder contraindication 38341003 DOID:10763
Chronic heart failure contraindication 48447003
Male hypogonadism contraindication 48723006
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Thromboembolic disorder contraindication 371039008
Adrenal cortical hypofunction contraindication 386584007 DOID:10493




๐Ÿถ Veterinary Drug Use

SpeciesUseRelation
Dogs Alleviation of false pregnancy Indication
Dogs Postponement of estrus Indication

๐Ÿถ Veterinary products

ProductApplicantIngredients
Ovaban Tablets 20 mg, Ovaban Tablets 5 mg Intervet Inc. 1

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
125MG/ML MEGACE ES ENDO PHARMS INC N021778 July 5, 2005 RX SUSPENSION ORAL 7101576 April 22, 2024 TREATMENT OF ANOREXIA, CACHEXIA, OR AN UNEXPLAINED, SIGNIFICANT WEIGHT LOSS IN PATIENTS WITH A DIAGNOSIS OF ACQUIRED IMMUNODEFICIENCY SYNDROME (AIDS)
125MG/ML MEGACE ES ENDO PHARMS INC N021778 July 5, 2005 RX SUSPENSION ORAL 9040088 April 22, 2024 TREATMENT OF ANOREXIA, CACHEXIA, OR AN UNEXPLAINED, SIGNIFICANT WEIGHT LOSS IN PATIENTS WITH A DIAGNOSIS OF ACQUIRED IMMUNODEFICIENCY SYNDROME (AIDS)
125MG/ML MEGACE ES ENDO PHARMS INC N021778 July 5, 2005 RX SUSPENSION ORAL 9101540 April 22, 2024 TREATMENT OF ANOREXIA, CACHEXIA, OR AN UNEXPLAINED, SIGNIFICANT WEIGHT LOSS IN PATIENTS WITH A DIAGNOSIS OF ACQUIRED IMMUNODEFICIENCY SYNDROME (AIDS)
125MG/ML MEGACE ES ENDO PHARMS INC N021778 July 5, 2005 RX SUSPENSION ORAL 9101549 April 22, 2024 TREATMENT OF ANOREXIA, CACHEXIA, OR AN UNEXPLAINED, SIGNIFICANT WEIGHT LOSS IN PATIENTS WITH A DIAGNOSIS OF ACQUIRED IMMUNODEFICIENCY SYNDROME (AIDS)
125MG/ML MEGACE ES ENDO PHARMS INC N021778 July 5, 2005 RX SUSPENSION ORAL 9107827 April 22, 2024 TREATMENT OF ANOREXIA, CACHEXIA, OR AN UNEXPLAINED, SIGNIFICANT WEIGHT LOSS IN PATIENTS WITH A DIAGNOSIS OF ACQUIRED IMMUNODEFICIENCY SYNDROME (AIDS)

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 DRUGBANK CHEMBL
Multidrug resistance protein 1 Transporter WOMBAT-PK
Glucocorticoid receptor Nuclear hormone receptor Ki 8.06 DRUG MATRIX
Cytochrome P450 2C9 Enzyme IC50 5 DRUG MATRIX
Androgen receptor Transcription factor Ki 7.70 DRUG MATRIX
Progesterone receptor Transcription factor Ki 8.84 DRUG MATRIX

External reference:

IDSource
4022205 VUID
N0000020211 NUI
D00952 KEGG_DRUG
4018133 VANDF
4022205 VANDF
C0065879 UMLSCUI
CHEBI:6723 CHEBI
CHEBI:6722 CHEBI
CHEMBL1201139 ChEMBL_ID
DB00351 DRUGBANK_ID
D019290 MESH_DESCRIPTOR_UI
11683 PUBCHEM_CID
9128 IUPHAR_LIGAND_ID
TJ2M0FR8ES UNII
29451 RXNORM
1784 MMSL
5036 MMSL
d01348 MMSL
002667 NDDF
004823 NDDF
126091007 SNOMEDCT_US
126092000 SNOMEDCT_US
38578004 SNOMEDCT_US
C0025175 UMLSCUI
1529 INN_ID
3562-63-8 SECONDARY_CAS_RN
D008535 MESH_DESCRIPTOR_UI
19090 PUBCHEM_CID
EA6LD1M70M UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0121-0887 SUSPENSION 625 mg ORAL ANDA 30 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0121-0945 SUSPENSION 400 mg ORAL ANDA 21 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0121-4776 SUSPENSION 40 mg ORAL ANDA 24 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0121-4776 SUSPENSION 40 mg ORAL ANDA 24 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0555-0606 TABLET 20 mg ORAL ANDA 20 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0555-0607 TABLET 40 mg ORAL ANDA 20 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0904-3571 TABLET 40 mg ORAL ANDA 19 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0904-7072 SUSPENSION 40 mg ORAL ANDA 22 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0904-7236 TABLET 40 mg ORAL ANDA 17 sections
Megace ES HUMAN PRESCRIPTION DRUG LABEL 1 16590-254 SUSPENSION 125 mg ORAL NDA 11 sections
MEGESTOL HUMAN PRESCRIPTION DRUG LABEL 1 16590-898 SUSPENSION 40 mg ORAL ANDA 4 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 17856-0060 SUSPENSION 40 mg ORAL ANDA 12 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 17856-0907 SUSPENSION 40 mg ORAL ANDA 20 sections
Megace ES HUMAN PRESCRIPTION DRUG LABEL 1 17856-0949 SUSPENSION 125 mg ORAL NDA 25 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 24979-041 SUSPENSION 125 mg ORAL ANDA 27 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 33358-903 SUSPENSION 40 mg ORAL ANDA 10 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 49884-230 SUSPENSION 125 mg ORAL NDA AUTHORIZED GENERIC 26 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 49884-230 SUSPENSION 125 mg ORAL NDA AUTHORIZED GENERIC 26 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 49884-289 TABLET 20 mg ORAL ANDA 19 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 49884-289 TABLET 20 mg ORAL ANDA 19 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 49884-290 TABLET 40 mg ORAL ANDA 19 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 49884-290 TABLET 40 mg ORAL ANDA 19 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 49884-907 SUSPENSION 40 mg ORAL ANDA 22 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 49884-907 SUSPENSION 40 mg ORAL ANDA 22 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 49884-907 SUSPENSION 40 mg ORAL ANDA 22 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 50383-859 SUSPENSION 40 mg ORAL ANDA 19 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 50383-859 SUSPENSION 40 mg ORAL ANDA 19 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 50383-859 SUSPENSION 40 mg ORAL ANDA 19 sections
Megestrol acetate HUMAN PRESCRIPTION DRUG LABEL 1 51991-313 SUSPENSION 125 mg ORAL ANDA 28 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 53808-0614 TABLET 40 mg ORAL ANDA 18 sections