Scroll

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

Stem definition	Drug id	CAS RN
steroids, progestogens	1667	595-33-5

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
5	mg	O
0.16	g	O

ADMET properties:

Property	Value	Reference
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)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
Aug. 18, 1971	FDA	BRISTOL MYERS SQUIBB

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Death	116.32	20.43	154	5499	374227	63109142
Decreased appetite	98.14	20.43	116	5537	250936	63232433
Malignant neoplasm progression	71.74	20.43	59	5594	82062	63401307
Neutropenia	68.48	20.43	81	5572	174924	63308445
Disease progression	56.77	20.43	62	5591	122696	63360673
Deep vein thrombosis	56.60	20.43	52	5601	83748	63399621
Metastases to liver	51.88	20.43	30	5623	23609	63459760
Dehydration	48.52	20.43	68	5585	173286	63310083
Asthenia	41.97	20.43	100	5553	383504	63099865
Diarrhoea	38.57	20.43	145	5508	715221	62768148
Metastases to bone	36.61	20.43	23	5630	20996	63462373
Hypoaesthesia oral	29.82	20.43	17	5636	13016	63470353
Abdominal pain	28.33	20.43	73	5580	293383	63189986
Oestrogen receptor assay positive	28.29	20.43	7	5646	505	63482864
Meningioma	27.41	20.43	11	5642	3874	63479495
Papillary thyroid cancer	25.43	20.43	9	5644	2247	63481122
Gastritis	24.86	20.43	23	5630	37280	63446089
Dysgeusia	24.04	20.43	25	5628	46685	63436684
Neutropenic sepsis	23.75	20.43	16	5637	16422	63466947
Breast cancer	23.31	20.43	25	5628	48358	63435011
Thoracic vertebral fracture	22.39	20.43	10	5643	4582	63478787
Anaemia	22.37	20.43	67	5586	293363	63190006
Nausea	21.83	20.43	140	5513	854331	62629038
Pulmonary embolism	21.74	20.43	38	5615	116646	63366723
Constipation	21.72	20.43	56	5597	224887	63258482

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	77.72	18.63	88	6327	87958	34862558
Death	76.80	18.63	201	6214	397848	34552668
Respiratory tract infection bacterial	75.19	18.63	23	6392	1759	34948757
Respiratory tract infection viral	71.32	18.63	24	6391	2493	34948023
Asthenia	68.08	18.63	143	6272	245108	34705408
Decreased appetite	65.93	18.63	113	6302	166279	34784237
Dehydration	63.35	18.63	97	6318	129872	34820644
Adrenal insufficiency	58.95	18.63	35	6380	14012	34936504
Pneumonia	54.94	18.63	168	6247	362459	34588057
Pulmonary embolism	52.41	18.63	73	6342	89673	34860843
Fatigue	44.68	18.63	159	6256	370494	34580022
Disease progression	38.31	18.63	70	6345	108007	34842509
Anaemia	35.07	18.63	108	6307	233227	34717289
Respiratory tract infection	32.97	18.63	28	6387	19684	34930832
Plasma cell myeloma	30.38	18.63	38	6377	41999	34908517
Diarrhoea	28.68	18.63	144	6271	389768	34560748
Drug ineffective	26.49	18.63	27	6388	456724	34493792
Weight decreased	23.16	18.63	78	6337	176223	34774293
Dysphagia	22.82	18.63	41	6374	62340	34888176
Platelet count decreased	21.36	18.63	59	6356	119658	34830858
Thrombocytopenia	21.29	18.63	70	6345	156177	34794339
Androgen deficiency	19.42	18.63	5	6410	203	34950313

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Death	130.76	17.59	231	8794	566283	79169080
Decreased appetite	110.77	17.59	163	8862	342255	79393108
Dehydration	97.85	17.59	130	8895	248057	79487306
Respiratory tract infection bacterial	82.68	17.59	23	9002	2054	79733309
Adrenal insufficiency	74.31	17.59	44	8981	28443	79706920
Malignant neoplasm progression	74.21	17.59	84	8941	135906	79599457
Pulmonary embolism	73.94	17.59	94	8931	171560	79563803
Asthenia	71.69	17.59	170	8855	511519	79223844
Respiratory tract infection viral	70.30	17.59	24	9001	4235	79731128
Pneumonia	69.54	17.59	197	8828	660049	79075314
Disease progression	54.08	17.59	84	8941	184278	79551085
Plasma cell myeloma	49.57	17.59	44	8981	53215	79682148
Anaemia	48.87	17.59	135	8890	444880	79290483
Neutropenia	46.15	17.59	101	8924	287609	79447754
Diarrhoea	44.63	17.59	207	8818	880282	78855081
Platelet count decreased	34.25	17.59	71	8954	194593	79540770
Deep vein thrombosis	33.90	17.59	54	8971	120865	79614498
Drug ineffective	33.68	17.59	44	8981	1080869	78654494
Fatigue	32.24	17.59	197	8828	929530	78805833
Thrombocytopenia	28.57	17.59	80	8945	265179	79470184
Respiratory tract infection	28.10	17.59	31	8994	48658	79686705
Constipation	26.31	17.59	81	8944	282969	79452394
Mental status changes	26.17	17.59	35	8990	66924	79668439
Pleural effusion	25.56	17.59	53	8972	145209	79590154
Androgen deficiency	25.13	17.59	5	9020	102	79735261
Failure to thrive	25.03	17.59	16	9009	11828	79723535
Meningioma	23.80	17.59	11	9014	4287	79731076
Blood testosterone decreased	22.87	17.59	9	9016	2368	79732995
Secondary adrenocortical insufficiency	20.80	17.59	9	9016	3005	79732358
Hypoaesthesia oral	20.19	17.59	15	9010	14109	79721254
Malnutrition	19.76	17.59	18	9007	22484	79712879
Hypophagia	19.73	17.59	25	9000	45342	79690021
Cachexia	18.66	17.59	13	9012	11070	79724293
Dysphagia	18.54	17.59	42	8983	122094	79613269
Lethargy	18.38	17.59	33	8992	81259	79654104
Dysgeusia	18.06	17.59	27	8998	57150	79678213
Sepsis	17.92	17.59	69	8956	269359	79466004
Toxicity to various agents	17.87	17.59	13	9012	421527	79313836

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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	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
FDA EPC	N0000175602	Progestin
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|

Disease	Relation	SNOMED_ID	DOID
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

Species	Use	Relation
Dogs	Alleviation of false pregnancy	Indication
Dogs	Postponement of estrus	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Progesterone receptor	Nuclear hormone receptor	P06401	PRGR_HUMAN	AGONIST			DRUGBANK	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN				WOMBAT-PK
Glucocorticoid receptor	Nuclear hormone receptor	P04150	GCR_HUMAN		Ki	8.06	DRUG MATRIX
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	5	DRUG MATRIX
Androgen receptor	Transcription factor		ANDR_RAT		Ki	7.70	DRUG MATRIX
Progesterone receptor	Transcription factor		Q690N0_BOVIN		Ki	8.84	DRUG MATRIX

External reference:

ID	Source
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
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
19090	PUBCHEM_CID
D008535	MESH_DESCRIPTOR_UI
9128	IUPHAR_LIGAND_ID
EA6LD1M70M	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	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	0904-7072	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	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