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Drug

D0869 | desogestrel

Molecular Formula C22H30O
Molecular Weight 310.5
Structure
State solid
Clearance The metabolic clearance rate of desogestrel is reported to be of about 2 ml/min/kg.[F4127]
Volume of distribution The apparent volume of distribution of desogestrel is of 1.5 L/kg.[F4127]
Route of elimination The elimination of desogestrel is found to be mainly renal corresponding to about 6 times the dose eliminated in the bile.[F4127] The elimination of desogestrel is only done as the metabolites and not as the unchanged drug and about 85% of the administered dose can be excreted as metabolites after 6-8 days.[T521]
Protein binding The main metabolite of desogestrel is mainly found bound to albumin and sex-hormone binding globulin. Around 96-98% of the administered dose of desogestrel is found bound to plasma proteins from which 40-70% is found bound to sex-hormone binding globulin.[F4127]
Half life The terminal half-life of desogestrel is determined to be of 30 hours.[F4127]
Absorption After oral administration, desogestrel is rapidly absorbed and it reaches a peak concentration of 2 ng/ml after 1.5 hours. The bioavailability of desogestrel is reported to be in the range of 60-80% and the reported AUC is of 3000 ng.h/ml.[F4127] Almost all the administered dose is modified to the active metabolite, [etonogestrel].[A176423]

G

G03FB10 Desogestrel and estrogen


[G03FB] Progestogens and estrogens, sequential preparations


[G03F] PROGESTOGENS AND ESTROGENS IN COMBINATION


[G03] SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM


[G] Genitourinary system and reproductive hormones

G03AC09 Desogestrel


[G03AC] Progestogens


[G03A] HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE


[G03] SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM


[G] Genitourinary system and reproductive hormones

G03AB05 Desogestrel and ethinylestradiol


[G03AB] Progestogens and estrogens, sequential preparations


[G03A] HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE


[G03] SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM


[G] Genitourinary system and reproductive hormones

G03AA09 Desogestrel and ethinylestradiol


[G03AA] Progestogens and estrogens, fixed combinations


[G03A] HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE


[G03] SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM


[G] Genitourinary system and reproductive hormones

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 22.29±2.11 human qHTS-HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 27.48 human HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL rat hepatocytes MMP assay Negative IC50 163

Pictogram Signal Statements Precautionary Statement Codes
Danger

Aggregated GHS information provided by 62 companies from 9 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


H360 (37.1%): May damage fertility or the unborn child [Danger Reproductive toxicity]


H400 (61.29%): Very toxic to aquatic life [Warning Hazardous to the aquatic environment, acute hazard]


H410 (90.32%): Very toxic to aquatic life with long lasting effects [Warning Hazardous to the aquatic environment, long-term hazard]


Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.


 P201, P202, P273, P281, P308+P313, P391, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)


  • (17alpha)-13-Ethyl-11-methylene-18,19-dinorpregn-4-en-20-yn-17-ol (8S,9S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-11-methylidene-1,2,3,6,7,8,9,10,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-ol 024D225
    13-Ethyl-11-methylene-18,19-dinor-17 alpha-pregn-4-en-20-yn-17-ol 13-Ethyl-11-methylene-18,19-dinor-17alpha-pregn-4-en-20-yn-17-ol 13-ethyl-11-methylene-18,19-dinorpregn-4-en-20-yn-17alpha-ol
    17alpha-ethynyl-11-methylidene-18a-homo-estr-4-en-17beta-ol 17alpha-ethynyl-13beta-ethyl-11-methylene-4-gonen-17-ol 18,19-Dinorpregn-4-en-20-yn-17-ol, 13-ethyl-11-methylene-, (17-alpha)-
    18,19-Dinorpregn-4-en-20-yn-17-ol, 13-ethyl-11-methylene-, (17alpha)- 54024-22-5 81K9V7M3A3
    AC-308 ACN-037024 AKOS015963198
    AS-13022 B4976 BCP18794
    BDBM50423510 C-19240 C07629
    C22H30O CAS-54024-22-5 CC-26355
    CHEBI:4453 CHEMBL1533 CS-3686
    CTK8F9084 Cerazette Certified Reference Material
    D02367 D4163 DB00304
    DESOGESTREL DSSTox_CID_2898 DSSTox_GSID_22898
    DSSTox_RID_76779 DTXSID6022898 Desogestrel (USAN/INN)
    Desogestrel [USAN:BAN:INN] Desogestrel [USAN:INN:BAN] Desogestrel for system suitability, European Pharmacopoeia (EP) Reference Standard;
    Desogestrel, British Pharmacopoeia (BP) Reference Standard Desogestrel, European Pharmacopoeia (EP) Reference Standard Desogestrel, Pharmaceutical Secondary Standard
    Desogestrel, United States Pharmacopeia (USP) Reference Standard Desogestrel, VETRANAL(TM), analytical standard Desogestrelum
    Desogestrelum [INN-Latin] EINECS 258-929-4 FT-0640213
    GTPL7065 HSDB 3593 HY-12516
    J-520217 LMST02030104 LS-62079
    NCGC00167449-01 ORG 2969 Org-2969
    Q415304 RPLCPCMSCLEKRS-BPIQYHPVSA-N SC-16229
    SCHEMBL41341 SR-01000883959 SR-01000883959-1
    SR-01000883959-2 Tox21_112453 UNII-81K9V7M3A3
    VA10694 ZINC4097416 desogen
    s4638

    DrugBank Name desogestrel
    DrugBank DB00304
    CAS Number 54024-22-5
    PubChem Compound 40973
    KEGG Compound ID C07629
    KEGG Drug D02367
    ChEBI 4453