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 |
|---|---|
|
Synonyms:
|
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)
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) | 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 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 | 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 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 | 77.24 | 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 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 | 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:
| 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 |
| 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|
| 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]) | Mechanism action | Bioact source | MoA 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:
| 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 |
| 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:
| 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 | 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 |