megestrol acetate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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) 2 Bocci G, Oprea TI, Benet LZ
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 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 100 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,MAP3K7,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,STK33,SYK,TEK,TTK,ZAP70 33
kinase-selectivity-class EIF2AK3,GRK2 2
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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 150.06 22.55 169 5990 456382 90165906
Decreased appetite 94.90 22.55 122 6037 376418 90245870
Malignant neoplasm progression 82.80 22.55 64 6095 106806 90515482
Neutropenia 74.81 22.55 84 6075 224820 90397468
Deep vein thrombosis 71.24 22.55 55 6104 91565 90530723
Disease progression 70.89 22.55 69 6090 156546 90465742
Dehydration 58.51 22.55 69 6090 194378 90427910
Diarrhoea 51.63 22.55 160 5999 939030 89683258
Metastases to liver 51.19 22.55 29 6130 28778 90593510
Asthenia 44.34 22.55 106 6053 533645 90088643
Meningioma 41.96 22.55 15 6144 5056 90617232
Oestrogen receptor assay positive 40.53 22.55 9 6150 533 90621755
Mineralocorticoid deficiency 34.39 22.55 4 6155 0 90622288
Metastases to bone 33.15 22.55 21 6138 25484 90596804
Anaemia 32.45 22.55 73 6086 352729 90269559
Hypoaesthesia oral 31.25 22.55 17 6142 15583 90606705
Nausea 31.11 22.55 153 6006 1110163 89512125
Abdominal pain 31.10 22.55 77 6082 395644 90226644
Gastritis 30.12 22.55 24 6135 41729 90580559
Pulmonary embolism 29.13 22.55 40 6119 130780 90491508
Breast cancer 28.72 22.55 26 6133 53735 90568553
Adrenal insufficiency 27.78 22.55 20 6139 29901 90592387
Dysgeusia 27.25 22.55 25 6134 52535 90569753
Papillary thyroid cancer 26.47 22.55 9 6150 2618 90619670
Neutropenic sepsis 26.27 22.55 16 6143 18114 90604174
Constipation 25.74 22.55 58 6101 280337 90341951
Weight decreased 24.80 22.55 69 6090 379841 90242447
Secondary adrenocortical insufficiency 23.58 22.55 8 6151 2310 90619978
Thoracic vertebral fracture 23.29 22.55 10 6149 5464 90616824

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
Death 84.32 19.97 215 6742 470970 42143408
Malignant neoplasm progression 81.10 19.97 94 6863 108306 42506072
Respiratory tract infection bacterial 80.61 19.97 24 6933 1885 42612493
Decreased appetite 77.96 19.97 124 6833 193013 42421365
Asthenia 75.67 19.97 151 6806 280642 42333736
Dehydration 72.90 19.97 102 6855 141665 42472713
Adrenal insufficiency 70.81 19.97 42 6915 18882 42595496
Respiratory tract infection viral 70.75 19.97 25 6932 3381 42610997
Pneumonia 67.60 19.97 185 6772 421964 42192414
Fatigue 49.11 19.97 169 6788 435472 42178906
Pulmonary embolism 45.69 19.97 75 6882 119537 42494841
Anaemia 41.87 19.97 120 6837 280158 42334220
Drug ineffective 35.06 19.97 31 6926 630166 41984212
Diarrhoea 34.98 19.97 158 6799 460691 42153687
Disease progression 32.39 19.97 72 6885 143584 42470794
Respiratory tract infection 30.72 19.97 29 6928 26293 42588085
Plasma cell myeloma 30.17 19.97 38 6919 47540 42566838
Thrombocytopenia 28.86 19.97 82 6875 190197 42424181
Weight decreased 28.09 19.97 86 6871 207862 42406516
Hypogonadism 25.94 19.97 11 6946 2423 42611955
Dysphagia 23.01 19.97 42 6915 72677 42541701
Platelet count decreased 22.24 19.97 61 6896 138520 42475858
Failure to thrive 20.72 19.97 15 6942 9407 42604971

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 168.51 19.56 257 9749 698612 109880681
Decreased appetite 120.05 19.56 179 9827 475667 110103626
Dehydration 118.69 19.56 136 9870 279375 110299918
Adrenal insufficiency 109.00 19.56 60 9946 42330 110536963
Respiratory tract infection bacterial 89.01 19.56 24 9982 2392 110576901
Pneumonia 83.71 19.56 219 9787 876495 109702798
Malignant neoplasm progression 82.68 19.56 90 9916 174477 110404816
Pulmonary embolism 80.42 19.56 98 9908 214376 110364917
Asthenia 79.33 19.56 185 9821 688814 109890479
Respiratory tract infection viral 71.82 19.56 25 9981 5853 110573440
Anaemia 65.19 19.56 149 9857 546937 110032356
Neutropenia 63.45 19.56 118 9888 374502 110204791
Diarrhoea 61.76 19.56 234 9772 1139271 109440022
Disease progression 54.59 19.56 87 9919 243947 110335346
Plasma cell myeloma 51.74 19.56 44 9962 62892 110516401
Deep vein thrombosis 44.59 19.56 59 9947 139828 110439465
Platelet count decreased 39.46 19.56 73 9933 230370 110348923
Hypogonadism 38.56 19.56 12 9994 1982 110577311
Thrombocytopenia 37.09 19.56 91 9915 348794 110230499
Fatigue 36.94 19.56 211 9795 1215747 109363546
Meningioma 36.17 19.56 15 9991 5650 110573643
Sepsis 34.39 19.56 85 9921 327261 110252032
Drug ineffective 34.38 19.56 53 9953 1520487 109058806
Secondary adrenocortical insufficiency 32.63 19.56 13 9993 4421 110574872
Pleural effusion 31.30 19.56 57 9949 177652 110401641
Blood testosterone decreased 30.56 19.56 11 9995 2837 110576456
Constipation 30.54 19.56 86 9920 357700 110221593
Failure to thrive 28.91 19.56 17 9989 13557 110565736
Mental status changes 28.83 19.56 35 9971 76087 110503206
Malnutrition 28.61 19.56 22 9984 27257 110552036
Respiratory tract infection 27.23 19.56 33 9973 71584 110507709
Mineralocorticoid deficiency 25.61 19.56 4 10002 23 110579270
Androgen deficiency 25.39 19.56 5 10001 122 110579171
Nausea 25.06 19.56 194 9812 1235496 109343797
Febrile neutropenia 22.16 19.56 71 9935 316696 110262597
Infusion related reaction 21.92 19.56 4 10002 381158 110198135
Cachexia 21.85 19.56 14 9992 12991 110566302
Lethargy 21.77 19.56 34 9972 93542 110485751
Condition aggravated 21.39 19.56 21 9985 734815 109844478
Hypophagia 21.24 19.56 25 9981 52601 110526692
Weight decreased 21.08 19.56 91 9915 467966 110111327
Hypoaesthesia oral 20.71 19.56 15 9991 16987 110562306
Abdominal pain 19.58 19.56 95 9911 512894 110066399

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
MeSH PA D000080066 Contraceptive Agents, Hormonal
MeSH PA D000970 Antineoplastic Agents
MeSH PA D003271 Contraceptive Agents, Female
MeSH PA D003278 Contraceptives, Oral, Hormonal
MeSH PA D003280 Contraceptives, Oral, Synthetic
MeSH PA D012102 Reproductive Control Agents
MeSH PA D018931 Antineoplastic Agents, Hormonal
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:49323 contraceptive drug
CHEBI has role CHEBI:49326 synthetic oral contraceptive
CHEBI has role CHEBI:50779 appetite enhancer
CHEBI has role CHEBI:59826 progestin
FDA EPC N0000175602 Progestin
MeSH PA D000697 Central Nervous System Stimulants
MeSH PA D019167 Appetite Stimulants

Related Drugs by ATC class:

G03AA Progestogens and estrogens, fixed combinations 17 drugs
chlormadinonedesogestreldienogestdrospirenoneestetrolestradiolethinylestradioletynodiolgestodenelevonorgestrellynestrenolmedroxyprogesterone show all 17 →
G03AB Progestogens and estrogens, sequential preparations 10 drugs
chlormadinonedesogestreldienogestestradiolethinylestradiolgestodenelevonorgestrellynestrenolnorethisteronenorgestimate
G03AC Progestogens 9 drugs
desogestreldrospirenoneetonogestrellevonorgestrellynestrenolmedroxyprogesteronenorethisteronenorgestrienonequingestanol acetate
G03DB Pregnadien derivatives 7 drugs
chlormadinonedemegestonedienogestdydrogesteronemedrogestonenomegestrolpromegestone
G03FA Progestogens and estrogens, fixed combinations 15 drugs
dienogestdrospirenonedydrogesteroneethisteroneetynodiolhydroxyprogesterone caproatelevonorgestrellynestrenolmedroxyprogesteronemethylestrenolonenorethisteronenorethynodrel show all 15 →
G03FB Progestogens and estrogens, sequential preparations 10 drugs
chlormadinonedesogestreldydrogesteronelevonorgestrellynestrenolmedrogestonemedroxyprogesteronenomegestrolnorethisteronetrimegestone
L02AB Progestogens 2 drugs
gestonoronemedroxyprogesterone

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




🐶 Veterinary Drug Use

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

🐶 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)

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 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
CHEMBL1201139 ChEMBL_ID
DB00351 DRUGBANK_ID
D019290 MESH_DESCRIPTOR_UI
11683 PUBCHEM_CID
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
CHEBI:6723 CHEBI
3562-63-8 SECONDARY_CAS_RN
19090 PUBCHEM_CID
9128 IUPHAR_LIGAND_ID
1529 INN_ID
D008535 MESH_DESCRIPTOR_UI
EA6LD1M70M UNII
CHEBI:6722 CHEBI
EA6LD1M70M INXIGHT DRUGS
TJ2M0FR8ES INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0116-4011 SUSPENSION 40 mg ORAL ANDA 24 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0116-4011 SUSPENSION 40 mg ORAL ANDA 24 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0121-0945 SUSPENSION 400 mg ORAL ANDA 21 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0121-1038 SUSPENSION 400 mg ORAL ANDA 21 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 0904-7236 TABLET 40 mg ORAL ANDA 17 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0904-7577 SUSPENSION 400 mg ORAL ANDA 21 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
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 26 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 33358-903 SUSPENSION 40 mg ORAL ANDA 10 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 50383-859 SUSPENSION 40 mg ORAL ANDA 19 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 51407-910 SUSPENSION 40 mg ORAL ANDA 12 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
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 60432-126 SUSPENSION 40 mg ORAL ANDA 23 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 60687-916 SUSPENSION 40 mg ORAL ANDA 19 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 64380-158 TABLET 20 mg ORAL ANDA 17 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 64380-159 TABLET 40 mg ORAL ANDA 17 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 64380-160 SUSPENSION 40 mg ORAL ANDA 12 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 68094-063 SUSPENSION 40 mg ORAL ANDA 22 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 68094-174 SUSPENSION 40 mg ORAL ANDA 21 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 68788-8714 SUSPENSION 40 mg ORAL ANDA 12 sections
Megestrol Acetate HUMAN PRESCRIPTION DRUG LABEL 1 69339-160 SUSPENSION 40 mg ORAL ANDA 12 sections
Megestrol Acetate Human Prescription Drug Label 1 70954-896 SUSPENSION 40 mg ORAL ANDA 19 sections