NORELGESTROMIN

Description

Norelgestromin, the progestin, is the active metabolite of norgestimate and is structurally related to 19-nortestosterone. Norgestimate and norelgestromin mimic the physiologic effects of progesterone at the progesterone receptor. Johnson & Johnson developed an adhesive female contraceptive patch that contains ethinylestradiol (0.75mg) and the progestogen norelgestromin (6mg). his product is a combination contraceptive acting via the inhibition gonadotropins. Its primary mechanism of action involves the suppression of ovulation, including changes in the cervical mucus and endometrium. The patch delivers a continuous flow of hormones through the skin and into the bloodstream. The contraceptive patch is available in countries worldwide.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Progesterone receptor 61	Agonist 2,678

Conditions

Condition	Modality	Targets	Highest Phase	Product
Pregnancy 65	Preventing		Approved 8,429	ORTHO EVRA
Pregnancy 65	Preventing		Approved 8,429	XULANE

C_max

Value	Dose	Co-administered	Analyte	Population
987 pg/mL	6 mg 1 times / day steady-state, transdermal	ETHINYL ESTRADIOL	NORELGESTROMIN plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
156702 pg × h/mL	6 mg 1 times / day steady-state, transdermal	ETHINYL ESTRADIOL	NORELGESTROMIN plasma	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
27.6 h	6 mg 1 times / day steady-state, transdermal	ETHINYL ESTRADIOL	NORELGESTROMIN plasma	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
3%			NORELGESTROMIN serum	Homo sapiens

Doses

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Dose	Population	Adverse events
150 ug 1 times / day multiple, transdermal Recommended	healthy, 28.7 n = 1672	Disc. AE: Application site reaction, Nausea...
6 mg 1 times / week multiple, transdermal Recommended	healthy	Disc. AE: Cardiovascular risk, Venous thromboembolism...

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AEs

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AE	Significance	Dose	Population
Breast discomfort	1% Disc. AE	150 ug 1 times / day multiple, transdermal Recommended	healthy, 28.7 n = 1672
Headache	1.1% Disc. AE	150 ug 1 times / day multiple, transdermal Recommended	healthy, 28.7 n = 1672
Emotional lability	1.5% Disc. AE	150 ug 1 times / day multiple, transdermal Recommended	healthy, 28.7 n = 1672
Nausea	1.8% Disc. AE	150 ug 1 times / day multiple, transdermal Recommended	healthy, 28.7 n = 1672
Application site reaction	1.9% Disc. AE	150 ug 1 times / day multiple, transdermal Recommended	healthy, 28.7 n = 1672

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Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1,737	substrate 1,037	substrate 1,217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
	CYP2B6 664 UGT1A1 418 CYP1A2 1,054 CYP2C19 991 CYP3A5 395 CYP2C8 693

Drug as victim

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Target	Modality	Activity
CYP3A5 395	substrate 3,367	inconclusive
CYP1A2 1,054	substrate 3,367	no
CYP2C19 991	substrate 3,367	no
CYP2C8 693	substrate 3,367	no
CYP2D6 1,217	substrate 3,367	no

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Sourcing

Sourcing

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Vendor/Aggregator	ID	URL
1PlusChem LLC	1P00DB4K
AK Scientific	3046AH
AbovChem LLC	HY-G0018
BLD Pharm	BD123562
BOC Sciences	53016-31-2

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PubMed

Title	Date	PubMed
No data available in table

Patents

Sample Use Guides

In Vivo Use Guide

Transdermal system: 150 mcg/day norelgestromin and 35 mcg/day ethinyl estradiol.

Route of Administration: Transdermal

In Vitro Use Guide

After 24h incubation of physiological concentrations of estrone sulfate 5 nM the inhibitory effect of norelgestromin (NGMN) (a metabolite of norgestimate) at concentrations of 5 nM, 0.5 uM and 50 uM was 43, 74 and 97%, respectively, in T-47D cells; 25, 57 and 96 respectively, in MCF-7 cells. Comparative studies using medroxyprogesterone acetate (MPA) showed that this progestin also has an inhibitory effect on sulfatase activity, but significantly less intense than that of NGMN. The inhibition for MPA at concentrations of 5 nM, 0.5 uM and 50 uM was 31, 47 and 61, respectively, for T-47D cells; 6, 20 and 63, respectively, for MCF-7 cells.