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

Stem definition	Drug id	CAS RN
steroids, progestogens	818	54024-22-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: Org 2969 desogestrel cerazette	A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents (ORAL CONTRACEPTIVES, COMBINED). Molecular weight: 310.48 Formula: C22H30O CLOGP: 5.50 LIPINSKI: 1 HAC: 1 HDO: 1 TPSA: 20.23 ALOGS: -5.01 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

Org 2969
desogestrel
cerazette

A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents (ORAL CONTRACEPTIVES, COMBINED).

Molecular weight: 310.48
Formula: C22H30O
CLOGP: 5.50
LIPINSKI: 1
HAC: 1
HDO: 1
TPSA: 20.23
ALOGS: -5.01
ROTB: 1

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	5 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.32 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.01 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Dec. 10, 1992	FDA	ORGANON USA INC

FDA Adverse Event Reporting System (Female)

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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
Pregnancy on oral contraceptive	75.18	19.81	19	8233	1018	63479752
Muscle injury	56.37	19.81	55	8197	65290	63415480
Folliculitis	54.79	19.81	56	8196	70261	63410509
Irritable bowel syndrome	54.24	19.81	60	8192	82352	63398418
Lower respiratory tract infection	47.05	19.81	71	8181	132236	63348534
Blister	42.42	19.81	67	8185	129747	63351023
Impaired healing	40.74	19.81	58	8194	102484	63378286
Meningioma	39.81	19.81	16	8236	3869	63476901
Hepatocellular injury	39.71	19.81	31	8221	27350	63453420
Gastrointestinal disorder	36.50	19.81	63	8189	131176	63349594

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FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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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
Pregnancy on oral contraceptive	80.75	22.83	18	7059	827	79736484
Muscle injury	60.33	22.83	43	7034	48518	79688793
Irritable bowel syndrome	57.14	22.83	46	7031	62195	79675116
Folliculitis	53.12	22.83	42	7035	55338	79681973
Blister	44.64	22.83	54	7023	119422	79617889
Lower respiratory tract infection	44.41	22.83	56	7021	129164	79608147
Lip swelling	39.17	22.83	31	7046	40880	79696431
Night sweats	38.52	22.83	34	7043	52061	79685250
Impaired healing	38.39	22.83	43	7034	87612	79649699
Peripheral venous disease	37.13	22.83	21	7056	15888	79721423

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	G03AA09	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	G03AB05	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	G03AC09	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE Progestogens
ATC	G03FB10	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM PROGESTOGENS AND ESTROGENS IN COMBINATION Progestogens and estrogens, sequential preparations
CHEBI has role	CHEBI:49323	contraceptive drugs
CHEBI has role	CHEBI:49326	synthetic oral contraceptives
CHEBI has role	CHEBI:59826	progestins
FDA CS	M0447349	Progesterone Congeners
FDA EPC	N0000175602	Progestin
MeSH PA	D003270	Contraceptive Agents

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

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Disease	Relation	SNOMED_ID	DOID
Contraception	indication	13197004
Amenorrhea	off-label use	14302001	DOID:13938
Female hypogonadism syndrome	off-label use	16041008
Polycystic ovaries	off-label use	69878008
Dysmenorrhea	off-label use	266599000
Abnormal uterine bleeding unrelated to menstrual cycle	off-label use	312984006
Menorrhagia	off-label use	386692008
Heart valve disorder	contraindication	368009	DOID:4079
Hyperlipoproteinemia	contraindication	3744001	DOID:1168
Hypocalcemia	contraindication	5291005

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.93	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Progesterone receptor	Nuclear hormone receptor	P06401	PRGR_HUMAN	AGONIST				WOMBAT-PK	CHEMBL
Sex hormone-binding globulin	Secreted	P04278	SHBG_HUMAN		Kd	6.60		CHEMBL

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External reference:

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ID	Source
003956	NDDF
116074007	SNOMEDCT_US
126108008	SNOMEDCT_US
22656	RXNORM
4020568	VUID
4020568	VANDF
40973	PUBCHEM_CID
4384	INN_ID
4549	MMSL
7065	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
MERCILON	HUMAN OTC DRUG LABEL	2	72689-0020	TABLET	0.15 mg	ORAL	unapproved drug other	7 sections

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