Identification

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Name
Desogestrel
Accession Number
DB00304  (APRD00762)
Type
Small Molecule
Groups
Approved
Description

Desogestrel, a prodrug, is a third generation progestogen1 and hence, a member of the gonane family which was largely used in Europe before being approved in the US and Canada.4 It was firstly generated from a study that showed that 11-beta and 11-alkylidene substituent in nortestosterone can enhance the biological activity.10 Desogestrel is now produced semi-synthetically from naturally occurred plant steroids.13 In the US, desogestrel is found only in combination with ethinyl estradiol.5 The first approved drug containing desogestrel was developed by Organon USA Inc in 1972 and FDA approved in 1992.11

Structure
Thumb
Synonyms
  • 13-Ethyl-11-methylene-18,19-dinor-17α-pregn-4-en-20-yn-17-ol
  • Desogestrel
  • Désogestrel
  • Desogestrelum
External IDs
ORG 2969 / ORG-2969
Product Images
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
ApriDesogestrel (0.15 mg/1) + Ethinylestradiol (0.03 mg/1)KitPhysicians Total Care, Inc.2003-03-10Not applicableUs54868 475420180907 15195 183ataj
Apri 21Desogestrel (0.15 mg) + Ethinylestradiol (0.03 mg)TabletOralTeva2008-09-29Not applicableCanada
Apri 28Desogestrel (0.15 mg) + Ethinylestradiol (0.03 mg)TabletOralTeva2008-09-29Not applicableCanada
Apri 28 DayDesogestrel (0.15 mg/1) + Ethinylestradiol (0.03 mg/1)KitTeva1999-10-22Not applicableUs00555 9043 58 nlmimage10 d5136aab
Apri 28 DayDesogestrel (0.15 mg/1) + Ethinylestradiol (0.03 mg/1)KitA-S Medication Solutions1999-10-22Not applicableUs
AzuretteDesogestrel (0.15 mg/1) + Ethinylestradiol (0.02 mg/1) + Ethinylestradiol (0.01 mg/1)KitMayne Pharma Inc.2016-11-14Not applicableUs
AzuretteDesogestrel (0.15 mg/1) + Ethinylestradiol (0.02 mg/1)KitRpk Pharmaceuticals, Inc.2016-11-14Not applicableUs
AzuretteDesogestrel (0.15 mg/1) + Ethinylestradiol (0.02 mg/1) + Ethinylestradiol (0.01 mg/1)KitActavis Pharma Company2008-12-302017-12-31Us52544 0940 28 nlmimage10 ad3ad6f6
BekyreeDesogestrel (0.15 mg/1) + Ethinylestradiol (0.02 mg/1) + Ethinylestradiol (0.01 mg/1)KitLupin Pharmaceuticals2015-10-26Not applicableUs
BekyreeDesogestrel (0.15 mg/1) + Ethinylestradiol (0.02 mg/1) + Ethinylestradiol (0.01 mg/1)KitLupin Pharmaceuticals2015-10-262019-08-01Us
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
MercilonDesogestrel (0.15 mg/1) + Ethinylestradiol (0.02 mg/1)TabletOralOASIS TRADING2018-11-22Not applicableUs
International/Other Brands
Cerazette (Organon) / Marvelon (Adcock Ingram Pharmaceuticals)
Categories
UNII
81K9V7M3A3
CAS number
54024-22-5
Weight
Average: 310.473
Monoisotopic: 310.229665582
Chemical Formula
C22H30O
InChI Key
RPLCPCMSCLEKRS-BPIQYHPVSA-N
InChI
InChI=1S/C22H30O/c1-4-21-14-15(3)20-17-9-7-6-8-16(17)10-11-18(20)19(21)12-13-22(21,23)5-2/h2,8,17-20,23H,3-4,6-7,9-14H2,1H3/t17-,18-,19-,20+,21-,22-/m0/s1
IUPAC Name
(1S,2R,10S,11S,14R,15S)-15-ethyl-14-ethynyl-17-methylidenetetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadec-6-en-14-ol
SMILES
[H][C@@]12CC[C@@](O)(C#C)[C@@]1(CC)CC(=C)[C@]1([H])[C@@]3([H])CCCC=C3CC[C@@]21[H]

Pharmacology

Indication

Oral desogestrel is used in combination with ethinylestradiol as a contraceptive agent for the prevention of pregnancy.Label

Desogestrel is part of the combined oral contraceptives that contain a mix of estrogen and progestin which inhibit ovulation.12

Associated Therapies
Pharmacodynamics

The effects of desogestrel are divided on reproductive including modification of luteinizing hormone and follicle stimulating hormone, declines on the onset of menstruation, and increases the viscosity of the vaginal fluid; and on metabolic that includes increase insulin secretion and resistance, increased lipase activity, and increased fat deposition.9 The effect of desogestrel on the lipids has been studied extensively and the results are contradictory.

Desogestrel main therapeutic effect due to its mechanism of action is known to be related to the inhibition of the ovulation in 97% of the cycles. This effect was proven in clinical trials in non-breastfeeding women from which the Pearl failure rate was reported to be of 0.17 per 100 women-years. This result indicated that desogestrel is more efficient when compared to other progestogen-only pills.6 All the therapeutic effect is produced by a transformation of the endometrium followed by an inhibition of the ovulation due to the suppression of other hormones.10

Desogestrel has been widely confirmed to be related to an increase in the risk of venous thromboembolism due to the driven increased in blood coagulation factors, leading to a pronounced prothrombotic state.1 However, the effects of desogestrel are known to not impact significantly the level of total cholesterol remaining in the range of change of 10% which allows it to be a molecule that presents a favorable lipid profile.4

Mechanism of action

Desogestrel enters the cell passively and acts by binding selectively to the progesterone receptor and generating low androgenic activity.8 Its binding produces an effect like a transcription factor and thus, it produces modifications in the mRNA synthesis.9

The active metabolite of desogestrel, etonogestrel, presents a combination of high progestational activity with minimal intrinsic androgenicity.Label

TargetActionsOrganism
AProgesterone receptor
agonist
Humans
AEstrogen receptor alpha
agonist
Humans
Additional Data Available
Adverse Effects

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

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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.13 Almost all the administered dose is modified to the active metabolite, etonogestrel.7

Volume of distribution

The apparent volume of distribution of desogestrel is of 1.5 L/kg.13

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.13

Metabolism

Desogestrel is rapidly metabolized in the intestinal mucosa and by first-pass hepatic metabolism8 to form the major metabolite of desogestrel is etonogestrel which is the biologically active metabolite.2,3 This modification is described by the hydroxylation in C3 of the desogestrel molecule.7 Later, etonogestrel is metabolized following the normal pathways of steroid metabolism. On the other hand, due to the 11-methylene side chain, desogestrel cannot be metabolized to other progestins.13

Route of elimination

The elimination of desogestrel is found to be mainly renal corresponding to about 6 times the dose eliminated in the bile.13 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.10

Half life

The terminal half-life of desogestrel is determined to be of 30 hours.13

Clearance

The metabolic clearance rate of desogestrel is reported to be of about 2 ml/min/kg.13

Toxicity

Administration of large quantities of desogestrel has been shown to produce strong hormonal effects but to lack chronic toxicity. The reported LD50 in rats after oral administration of desogestrel is higher than 2000 mg/kg.10 Overdose hasn't reported serious effects but only symptoms of nausea and withdrawal of bleeding.Label

Most reports haven't linked the administration of desogestrel with the increased risk of breast cancer. The increased risk has been reported to be related to the duration of use. However, several reports indicate a desogestrel-driven increased risk in cervical intra-epithelial neoplasia but the results are still not conclusive.Label

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinDesogestrel may decrease the anticoagulant activities of (R)-warfarin.
(S)-WarfarinDesogestrel may decrease the anticoagulant activities of (S)-Warfarin.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Desogestrel.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Desogestrel.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Desogestrel.
4-OxoretinolThe therapeutic efficacy of Desogestrel can be decreased when used in combination with 4-Oxoretinol.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Desogestrel.
6-Deoxyerythronolide BThe metabolism of Desogestrel can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Desogestrel.
7-ethyl-10-hydroxycamptothecinThe metabolism of Desogestrel can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
Additional Data Available
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    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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    Severity

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  • Evidence Level
    Evidence Level

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Food Interactions
Not Available

References

Synthesis Reference
US20130123523
General References
  1. Park MJ, Jeon GH: Pulmonary embolism in a healthy woman using the oral contraceptives containing desogestrel. Obstet Gynecol Sci. 2017 Mar;60(2):232-235. doi: 10.5468/ogs.2017.60.2.232. Epub 2017 Mar 16. [PubMed:28344968]
  2. Schrager S, Paddock E, Dalby J, Knudsen L: Contraception in Wisconsin: a review. WMJ. 2010 Dec;109(6):326-31. [PubMed:21287884]
  3. Shimoni N, Westhoff C: Review of the vaginal contraceptive ring (NuvaRing). J Fam Plann Reprod Health Care. 2008 Oct;34(4):247-50. doi: 10.1783/147118908786000370. [PubMed:18854070]
  4. Laurendeau L: [Desogestrel contraceptives: the perfect pill for lipids?]. Can Fam Physician. 1996 Jan;42:62-71. [PubMed:8924815]
  5. Authors unspecified: Desogestrel . [PubMed:30000422]
  6. Guillebaud J: CEU New Product Review of the desogestrel-only pill. J Fam Plann Reprod Health Care. 2004 Jan;30(1):64; author reply 64-5. [PubMed:15006321]
  7. McClamrock HD, Adashi EY: Pharmacokinetics of desogestrel. Am J Obstet Gynecol. 1993 Mar;168(3 Pt 2):1021-8. [PubMed:8447355]
  8. Lemke T., Williams D., Roche V. and Zito W. (2008). Foye's Principles of Medicinal Chemistry (6th) (6th ed.). Lippincott Williams & Wilkins. [ISBN:978-0-7817-6879-5]
  9. Bardal S, Waechter J, Martin D. (2011). Applied Pharmacology. Elsevier Health Sciences. [ISBN:978-1-4377-0310-8]
  10. Runnebaum B., Rabe K. and Kiesel L. (1988). Female contraception. Springer-Verlag. [ISBN:978-3-642-73792-3]
  11. FDA approvals [Link]
  12. NIH [Link]
  13. MADELINE (desogestrel and ethinyl estradiol) Australian monograph [File]
External Links
Human Metabolome Database
HMDB0014449
KEGG Drug
D02367
KEGG Compound
C07629
PubChem Compound
40973
PubChem Substance
46505739
ChemSpider
37400
BindingDB
50423510
ChEBI
4453
ChEMBL
CHEMBL1533
Therapeutic Targets Database
DAP001209
PharmGKB
PA449238
Wikipedia
Desogestrel
ATC Codes
G03AA09 — Desogestrel and ethinylestradiolG03AB05 — Desogestrel and ethinylestradiolG03AC09 — DesogestrelG03FB10 — Desogestrel and estrogen
FDA label
Download (653 KB)
MSDS
Download (99.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedOtherBiological Availability1
1, 2CompletedTreatmentOvarian Stimulation1
2CompletedBasic ScienceHemostasis / Oral Contraceptives (OC)1
2CompletedTreatmentHealthy Volunteers1
2Unknown StatusTreatmentWomen With PMS1
2, 3CompletedTreatmentOndine Syndrome1
3Active Not RecruitingTreatmentDysfunctional Uterine Bleeding1
3CompletedPreventionContraception2
3CompletedTreatmentHealthy Volunteers1
3RecruitingTreatmentExercise-related Amenorrhea1
3RecruitingTreatmentInfertility, Female / Polycystic Ovaries Syndrome1
4Active Not RecruitingBasic ScienceOther Disorders of Bone Development and Growth1
4CompletedBasic ScienceBone; Disorder, Development and Growth1
4CompletedTreatmentInfertilities1
4CompletedTreatmentPremenstrual Syndrome1
4RecruitingTreatmentAdverse Effect of Oral Contraceptives, Sequela1
4TerminatedNot AvailableInfertilities1
4Unknown StatusDiagnosticBleeding1
4Unknown StatusTreatmentMenstrual Problem1
4Unknown StatusTreatmentUterine Leiomyomas1
4WithdrawnTreatmentInfertilities2
Not AvailableCompletedNot AvailableContraception1
Not AvailableCompletedNot AvailableContraceptive Usage / Vaginal Epithelial Disruption1
Not AvailableCompletedNot AvailableControlled Ovaria Stimulation1
Not AvailableCompletedNot AvailableFemale Sexual Function1
Not AvailableCompletedHealth Services ResearchOvarian Follicle1
Not AvailableCompletedTreatmentContraception1
Not AvailableCompletedTreatmentEndometriosis1
Not AvailableTerminatedTreatmentIn-Vitro Fertilization / Infertilities1
Not AvailableUnknown StatusTreatmentCongenital Central Hypoventilation Syndrome1
Not AvailableUnknown StatusTreatmentEndometriosis / Pain NOS1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Organon Pharmaceuticals
Dosage forms
FormRouteStrength
Kit
TabletOral
Prices
Unit descriptionCostUnit
Mircette 28 0.15-0.02/0.01 mg (21/5) tablet Disp Pack79.99USD disp
Kariva 28 0.15-0.02/0.01 mg (21/5) tablet Disp Pack62.38USD disp
Cyclessa 28 tablet Disp Pack56.39USD disp
Desogen 28 day tablet1.86USD tablet
Cyclessa 28 day tablet1.82USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)109-110ºCVan den Broek, A.J.; US. Patent 3,927,046; December 16, 1975; assigned to Akzona, Inc.
boiling point (°C)428ºCChemicalBook
water solubility<1 mg/mlMADELINE (desogestrel and ethinyl estradiol) Australian monograph
logP5.65'MSDS'
pKa13.04ChemicalBook
Predicted Properties
PropertyValueSource
Water Solubility0.00301 mg/mLALOGPS
logP4.3ALOGPS
logP4.42ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)17.99ChemAxon
pKa (Strongest Basic)-1.5ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area20.23 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity95.73 m3·mol-1ChemAxon
Polarizability37.54 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9941
Blood Brain Barrier+0.9619
Caco-2 permeable+0.774
P-glycoprotein substrateSubstrate0.6665
P-glycoprotein inhibitor IInhibitor0.6013
P-glycoprotein inhibitor IINon-inhibitor0.8924
Renal organic cation transporterNon-inhibitor0.7478
CYP450 2C9 substrateNon-substrate0.8183
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.6794
CYP450 1A2 substrateNon-inhibitor0.8353
CYP450 2C9 inhibitorNon-inhibitor0.7484
CYP450 2D6 inhibitorNon-inhibitor0.9132
CYP450 2C19 inhibitorInhibitor0.8537
CYP450 3A4 inhibitorNon-inhibitor0.764
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6204
Ames testNon AMES toxic0.923
CarcinogenicityNon-carcinogens0.9213
BiodegradationNot ready biodegradable0.9935
Rat acute toxicity2.3315 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7135
hERG inhibition (predictor II)Non-inhibitor0.7626
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as estrane steroids. These are steroids with a structure based on the estrane skeleton.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Estrane steroids
Direct Parent
Estrane steroids
Alternative Parents
17-hydroxysteroids / Delta-4-steroids / Ynones / Tertiary alcohols / Cyclic alcohols and derivatives / Acetylides / Hydrocarbon derivatives
Substituents
17-hydroxysteroid / Hydroxysteroid / Estrane-skeleton / Delta-4-steroid / Ynone / Tertiary alcohol / Cyclic alcohol / Acetylide / Organic oxygen compound / Hydrocarbon derivative
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
terminal acetylenic compound, 17beta-hydroxy steroid (CHEBI:4453) / C21 steroids (gluco/mineralocorticoids, progestogens) and derivatives (C07629) / C21 steroids (gluco/mineralocorticoids, progestogins) and derivatives (LMST02030104)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
Gene Name
PGR
Uniprot ID
P06401
Uniprot Name
Progesterone receptor
Molecular Weight
98979.96 Da
References
  1. Bergink EW, van Meel F, Turpijn EW, van der Vies J: Binding of progestagens to receptor proteins in MCF-7 cells. J Steroid Biochem. 1983 Nov;19(5):1563-70. [PubMed:6645495]
  2. Fuhrmann U, Slater EP, Fritzemeier KH: Characterization of the novel progestin gestodene by receptor binding studies and transactivation assays. Contraception. 1995 Jan;51(1):45-52. [PubMed:7750284]
  3. Kloosterboer HJ, Vonk-Noordegraaf CA, Turpijn EW: Selectivity in progesterone and androgen receptor binding of progestagens used in oral contraceptives. Contraception. 1988 Sep;38(3):325-32. [PubMed:3139361]
  4. Macpherson AM, Archer DF, Leslie S, Charnock-Jones DS, Makkink WK, Smith SK: The effect of etonogestrel on VEGF, oestrogen and progesterone receptor immunoreactivity and endothelial cell number in human endometrium. Hum Reprod. 1999 Dec;14(12):3080-7. [PubMed:10601100]
  5. Charnock-Jones DS, Macpherson AM, Archer DF, Leslie S, Makkink WK, Sharkey AM, Smith SK: The effect of progestins on vascular endothelial growth factor, oestrogen receptor and progesterone receptor immunoreactivity and endothelial cell density in human endometrium. Hum Reprod. 2000 Aug;15 Suppl 3:85-95. [PubMed:11041225]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
Gene Name
ESR1
Uniprot ID
P03372
Uniprot Name
Estrogen receptor
Molecular Weight
66215.45 Da
References
  1. Fuhrmann U, Slater EP, Fritzemeier KH: Characterization of the novel progestin gestodene by receptor binding studies and transactivation assays. Contraception. 1995 Jan;51(1):45-52. [PubMed:7750284]
  2. Rabe T, Bohlmann MK, Rehberger-Schneider S, Prifti S: Induction of estrogen receptor-alpha and -beta activities by synthetic progestins. Gynecol Endocrinol. 2000 Apr;14(2):118-26. [PubMed:10836199]
  3. Juchem M, Pollow K: Binding of oral contraceptive progestogens to serum proteins and cytoplasmic receptor. Am J Obstet Gynecol. 1990 Dec;163(6 Pt 2):2171-83. [PubMed:2175153]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Korhonen T, Tolonen A, Uusitalo J, Lundgren S, Jalonen J, Laine K: The role of CYP2C and CYP3A in the disposition of 3-keto-desogestrel after administration of desogestrel. Br J Clin Pharmacol. 2005 Jul;60(1):69-75. [PubMed:15963096]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Lemke T., Williams D., Roche V. and Zito W. (2008). Foye's Principles of Medicinal Chemistry (6th) (6th ed.). Lippincott Williams & Wilkins. [ISBN:978-0-7817-6879-5]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inducer
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. MADELINE (desogestrel and ethinyl estradiol) Australian monograph [File]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Androgen binding
Specific Function
Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone...
Gene Name
SHBG
Uniprot ID
P04278
Uniprot Name
Sex hormone-binding globulin
Molecular Weight
43778.755 Da
References
  1. MADELINE (desogestrel and ethinyl estradiol) Australian monograph [File]

Drug created on June 13, 2005 07:24 / Updated on May 01, 2019 08:26