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 102.08 20.21 142 4868 325237 50274877
Decreased appetite 85.31 20.21 102 4908 200821 50399293
Neutropenia 64.15 20.21 76 4934 147889 50452225
Malignant neoplasm progression 61.16 20.21 52 4958 68072 50532042
Disease progression 53.11 20.21 56 4954 95810 50504304
Metastases to liver 50.75 20.21 29 4981 20075 50580039
Deep vein thrombosis 48.22 20.21 47 4963 73257 50526857
Dehydration 46.73 20.21 66 4944 152383 50447731
Asthenia 40.49 20.21 94 4916 318948 50281166
Metastases to bone 37.66 20.21 23 4987 17972 50582142
Diarrhoea 30.71 20.21 127 4883 588349 50011765
Oestrogen receptor assay positive 28.56 20.21 7 5003 436 50599678
Papillary thyroid cancer 25.49 20.21 9 5001 2006 50598108
Meningioma 24.12 20.21 10 5000 3439 50596675
Breast cancer 23.61 20.21 25 4985 42865 50557249
Thoracic vertebral fracture 22.52 20.21 10 5000 4063 50596051
Weight decreased 21.50 20.21 59 4951 221186 50378928
Plasma cell myeloma 20.41 20.21 20 4990 31302 50568812

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
Malignant neoplasm progression 77.24 19.50 84 5826 73775 29494842
Death 69.73 19.50 186 5724 341898 29226719
Dehydration 63.41 19.50 95 5815 114653 29453964
Asthenia 63.14 19.50 135 5775 215115 29353502
Decreased appetite 60.78 19.50 106 5804 145236 29423381
Adrenal insufficiency 50.38 19.50 30 5880 11084 29557533
Pneumonia 49.57 19.50 158 5752 320014 29248603
Fatigue 46.01 19.50 153 5757 316668 29251949
Disease progression 41.20 19.50 65 5845 81851 29486766
Plasma cell myeloma 31.58 19.50 38 5872 37077 29531540
Diarrhoea 30.45 19.50 139 5771 332559 29236058
Anaemia 24.65 19.50 92 5818 200859 29367758
Dysphagia 24.09 19.50 41 5869 54885 29513732
Weight decreased 20.97 19.50 72 5838 150833 29417784
Pulmonary embolism 20.03 19.50 46 5864 76488 29492129

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
Death 109.47 18.35 207 7877 482498 64008150
Dehydration 96.64 18.35 127 7957 216636 64274012
Decreased appetite 96.05 18.35 145 7939 281144 64209504
Asthenia 69.19 18.35 160 7924 427884 64062764
Adrenal insufficiency 69.01 18.35 40 8044 22447 64468201
Malignant neoplasm progression 64.48 18.35 75 8009 112796 64377852
Pneumonia 56.77 18.35 176 7908 559400 63931248
Disease progression 52.47 18.35 76 8008 141604 64349044
Plasma cell myeloma 51.22 18.35 44 8040 46031 64444617
Diarrhoea 39.72 18.35 187 7897 722517 63768131
Pulmonary embolism 35.71 18.35 65 8019 146291 64344357
Anaemia 34.52 18.35 115 7969 378565 64112083
Fatigue 33.56 18.35 183 7901 748547 63742101
Neutropenia 31.58 18.35 83 8001 239541 64251107
Deep vein thrombosis 31.27 18.35 51 8033 105131 64385517
Drug ineffective 29.90 18.35 37 8047 840210 63650438
Androgen deficiency 24.62 18.35 5 8079 102 64490546
Pleural effusion 24.50 18.35 51 8033 126508 64364140
Mental status changes 24.36 18.35 34 8050 61128 64429520
Constipation 23.90 18.35 73 8011 229264 64261384
Failure to thrive 22.96 18.35 15 8069 10389 64480259
Blood testosterone decreased 22.95 18.35 9 8075 2116 64488532
Meningioma 20.72 18.35 10 8074 3872 64486776
Cachexia 19.63 18.35 13 8071 9204 64481444
Secondary adrenocortical insufficiency 18.73 18.35 8 8076 2337 64488311
Malnutrition 18.71 18.35 17 8067 19108 64471540

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
3562-63-8 SECONDARY_CAS_RN
TJ2M0FR8ES UNII
19090 PUBCHEM_CID
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
D008535 MESH_DESCRIPTOR_UI
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 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 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
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 54868-1629 TABLET 40 mg ORAL ANDA 19 sections
MEGESTROL ACETATE HUMAN PRESCRIPTION DRUG LABEL 1 54868-5389 SUSPENSION 40 mg ORAL ANDA 24 sections
MEGACE ES HUMAN PRESCRIPTION DRUG LABEL 1 54868-5572 SUSPENSION 125 mg ORAL NDA 27 sections