Delving into the Latest Updates on Ethinyl Estradiol/Norgestimate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Ethinylestradiol/norgestimate oral, NORGESTIMATE/ETHINYL ESTRADIOL, Ortho Tri-Cyclen

+ [18]

Target

ER x PR

Action

agonists

Mechanism

ERs agonists(Estrogen receptors agonists), PR agonists(Progesterone receptor agonists)

Therapeutic Areas

Other Diseases

Active Indication

Contraception

Inactive Indication

HemorrhageMetrorrhagia

Originator Organization

Johnson & Johnson

Active Organization

Ortho-McNeil Pharmaceutical LLC

Inactive Organization

Janssen Pharmaceuticals, Inc.

McNeil Consumer & Specialty Pharmaceuticals, Inc.Johnson & Johnson Pharmaceutical Research & Development LLC

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (29 Dec 1989),

Contraception

Regulation-

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Structure/Sequence

Molecular FormulaC43H55NO5

InChIKeyGYMWQLRSSDFGEQ-CXNPBKRFSA-N

CAS Registry79871-54-8

The purpose of the study is to evaluate the effect of VX-407 on the pharmacokinetics of levonorgestrel (LNG) and ethinyl estradiol (EE), norgestimate (NGM) and EE, norethindrone (NET) and EE and drospirenone (DRSP) and EE. Also, to evaluate the safety and tolerability of co-administration of VX-407 with LNG/EE, NGM/EE, NET/EE and DRSP/EE.

Start Date11 Jul 2025

Sponsor / Collaborator

Vertex Pharmaceuticals, Inc.

NCT06820307

/ CompletedPhase 1

A Phase 1, Open-label Study to Evaluate the Effect of Suzetrigine on the Pharmacokinetics of Oral Contraceptives in Healthy Female Subjects

The purpose of this study is to evaluate the effect of SUZ on the pharmacokinetics of oral contraceptives.

Start Date25 Feb 2025

Sponsor / Collaborator

Vertex Pharmaceuticals, Inc.

NCT04828824

/ RecruitingPhase 4IIT

Reduction of Premature Discontinuation of Contraceptive Implants by Advance Provision of an OCP-based Participant Intervention: Randomized Clinical Trial

To compare rates of etonogestrel implant discontinuation in implant initiators who are given advance provision of combined oral contraceptive pills (COCs) and a bleeding rescue regimen (COCR intervention) to participants given standard counseling (comparator).

Start Date18 Jun 2021

Sponsor / Collaborator

University of Colorado Denver

100 Clinical Results associated with Ethinyl Estradiol/Norgestimate

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100 Translational Medicine associated with Ethinyl Estradiol/Norgestimate

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100 Patents (Medical) associated with Ethinyl Estradiol/Norgestimate

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107

Literatures (Medical) associated with Ethinyl Estradiol/Norgestimate

01 Aug 2022·PHARMACEUTICAL CHEMISTRY JOURNAL

Validation of the Specificity of Chromatographic Methods: Key Points and Practical Recommendations

Author: Epshtein, N. A.

Specificity is one of the main tasks in reliable validation of anal. methods.Experience has shown that this problem is often treated rather formally in the case of using chromatog. methods for the determination of organic impurities so that the specificity of a proposed method is not fully proven.This article discusses key points for reliable assessment of the specificity of methods used for determining impurities.Practical recommendations and numerical values for decision making are given.The specificity of a method must be tested by conducting stress testing in such a way that the given API under stress degrades, i.e., the content of drug in the primary substance decreases, by greater than 0.5%.This is necessary at a min. for noticing the growth of existing impurities in the API and the formation of new impurities.On the other hand, the API degradation should not exceed 2% under oxidative stress and photodegradation conditions and should not exceed 5% for other stress factors (so as to minimize secondary reactions).The condition of permissible overlap of impurity peaks in the validation of method specificity has been substantiated as follows: the peak-to-valley (p/v) ratio should be ≥1.5 for overlapping impurity peaks.This is usually sufficient for ensuring reproducibility of the overlapping peak areas.If the overlapping peaks are close in height, then the p/v ratio can be <1.5 provided that the relative standard deviation of the area of overlapping peaks does not exceed 6% for successive injections (RSD ∼ 6%).This condition corresponds to a baseline signal-to-noise ratio S/N = 10, i.e., the limit of quantification.Issues related to validation of the specificity of methods for determining impurities in combined drugs are considered.

01 Jun 2019·Journal of applied physiology (Bethesda, Md. : 1985)Q3 · MEDICINE

Menstrual cycle-associated modulations in neuromuscular function and fatigability of the knee extensors in eumenorrheic women

Q3 · MEDICINE

Article

Author: Hicks, Kirsty M. ; Hunter, Sandra K. ; Simoes, Davina C. M. ; Howatson, Glyn ; Brownstein, Callum G. ; Goodall, Stuart ; Ansdell, Paul ; Škarabot, Jakob ; Thomas, Kevin

Sex hormone concentrations of eumenorrheic women typically fluctuate across the menstrual cycle and can affect neural function such that estrogen has neuroexcitatory effects, and progesterone induces inhibition. However, the effects of these changes on corticospinal and intracortical circuitry and the motor performance of the knee extensors are unknown. The present two-part investigation aimed to 1) determine the measurement error of an exercise task, transcranial magnetic stimulation (TMS)-, and motor nerve stimulation (MNS)-derived responses in women ingesting a monophasic oral contraceptive pill (hormonally-constant) and 2) investigate whether these measures were modulated by menstrual cycle phase (MCP), by examining them before and after an intermittent isometric fatiguing task (60% of maximal voluntary contraction, MVC) with the knee extensors until task failure in eumenorrheic women on days 2, 14, and 21 of the menstrual cycle. The repeatability of neuromuscular measures at baseline and fatigability ranged between moderate and excellent in women taking the oral contraceptive pill. MVC was not affected by MCP ( P = 0.790). Voluntary activation (MNS and TMS) peaked on day 14 ( P = 0.007 and 0.008, respectively). Whereas corticospinal excitability was unchanged, short-interval intracortical inhibition was greatest on day 21 compared with days 14 and 2 ( P < 0.001). Additionally, time to task failure was longer on day 21 than on both days 14 and 2 (24 and 36%, respectively, P = 0.030). The observed changes were larger than the associated measurement errors. These data demonstrate that neuromuscular function and fatigability of the knee extensors vary across the menstrual cycle and may influence exercise performance involving locomotor muscles. NEW & NOTEWORTHY The present two-part study first demonstrated the repeatability of transcranial magnetic stimulation- and electrical motor nerve stimulation-evoked variables in a hormonally constant female population. Subsequently, it was demonstrated that the eumenorrheic menstrual cycle affects neuromuscular function. Changing concentrations of neuroactive hormones corresponded to greater voluntary activation on day 14, greater intracortical inhibition on day 21, and lowest fatigability on day 21. These alterations of knee extensor neuromuscular function have implications for locomotor activities.

01 Nov 2017·Clinical pharmacokineticsQ2 · MEDICINE

No Dose Adjustment is Recommended for Digoxin, Warfarin, Atorvastatin or a Combination Oral Contraceptive When Coadministered with Dulaglutide

Q2 · MEDICINE

Article

Author: Geiser, Jeanne ; Loghin, Corina ; Cui, Xuewei ; de la Peña, Amparo

BACKGROUND:

Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) for the treatment of type 2 diabetes mellitus are known to delay gastric emptying (GE). The potential effect of the GLP-1 RA dulaglutide on the pharmacokinetics (PK) of four orally administered drugs and on the pharmacodynamic (PD) effect of warfarin was investigated.

METHODS:

In four separate clinical pharmacology studies, digoxin, warfarin, atorvastatin and Ortho-Cyclen^® were orally administered to healthy subjects with and without a subcutaneous dose of dulaglutide 1.5 mg. The effect of dulaglutide coadministration was assessed based on the PK parameters of key analytes. For warfarin PD, the effect of dulaglutide on the international normalized ratio (INR) was evaluated.

RESULTS:

Areas under the concentration-time curves (AUCs) with and without dulaglutide were similar for all analytes except atorvastatin, where it was reduced by 21%. Maximum concentrations (C _max) were generally lower following coadministration with dulaglutide, with statistically significant reductions (90% confidence intervals of geometric least squares means ratios outside 0.80-1.25) for all analytes except R-warfarin. For all analytes, there was a general trend for the time to C _max (t _max) to increase following coadministration with dulaglutide. For warfarin, dulaglutide coadministration had no statistically significant effect on the maximum INR (INR_max); however, a 2% increase in area under the INR curve (AUC_INR) was observed.

CONCLUSIONS:

Dulaglutide did not affect the absorption of the tested medications to a clinically relevant degree. Based on the PK and PD evaluations, no dose adjustments for digoxin, warfarin, atorvastatin and Ortho-Cyclen^® are recommended when coadministered with dulaglutide.

CLINICAL TRIAL REGISTRATION NUMBERS:

NCT01458210, NCT01436201, NCT01432938, and NCT01250834.

1

News (Medical) associated with Ethinyl Estradiol/Norgestimate

04 Mar 2021

·www.biospace.com

Mayne Pharma launches another generic oral contraceptive

ADELAIDE, Australia, March 4, 2021 /PRNewswire/ -- Mayne Pharma Group Limited (ASX: MYX) is pleased to announce the commercial launch of a generic version of ORTHO-CEPT® (desogestrel and ethinyl estradiol 0.15 mg / 0.03 mg) tablets to customers in the US. This is the fourth oral contraceptive launched this calendar year after launching generic versions of LOESTRIN® 24 FE, ORTHO CYCLEN® and ORTHO TRI-CYCLEN®. According to IQVIA, the annual US market sales for the four products were approximately US$315 million in the twelve months ending January 2021[1]. Mayne Pharma's CEO Scott Richards said, "We are very pleased to expand our Women's Health portfolio which now covers ~80% of Obstetrician/Gynaecologist oral contraceptive prescription volumes[1] and includes 24 marketed branded generic contraceptives. Mayne Pharma is committed to helping meet the needs of women in the US by providing cost effective, high-quality and novel contraceptive options. The four new products launched this year were sourced from the strategic partnership with Novast Laboratories." "In addition, Mayne Pharma has four women's health pipeline products pending at the FDA including the novel combined oral contraceptive NEXTSTELLIS™ (E4/DRSP) and a generic version of NUVARING®. NEXTSTELLIS which has a FDA target action date in April contains a new estrogen called estetrol or E4 in combination with a progestin, drospirenone. If approved, E4 will be the first new estrogen introduced in the US for contraceptive use in approximately 50 years." About Mayne Pharma Mayne Pharma is an ASX-listed specialty pharmaceutical company focused on applying its drug delivery expertise to commercialise branded and generic pharmaceuticals, offering patients better and more accessible medicines. Mayne Pharma also provides contract development and manufacturing services to more than 100 clients worldwide. Mayne Pharma has a 40-year track record of innovation and success in developing new oral drug delivery systems and these technologies have been successfully commercialised in numerous products that continue to be marketed around the world. Mayne Pharma has two facilities based in Salisbury, Australia and Greenville, USA with expertise in the formulation of complex oral and topical dose forms including potent compounds, modified-release products and poorly soluble compounds. LOESTRIN® 24 FE, NEXTSTELLIS™, NUVARING®, ORTHO-CEPT®, ORTHO CYCLEN® and ORTHO TRI-CYCLEN® are registered trademarks of third parties. [1] IQVIA, MAT Sales and NSP Units for brand and generic equivalents, January 2021 Company Codes: Australia:MYX, OTC-PINK:MYPHY

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100 Deals associated with Ethinyl Estradiol/Norgestimate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	G03AA11 G03AB09	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Contraception	United States	Janssen Pharmaceuticals, Inc.	29 Dec 1989

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hemorrhage	Phase 2	-	McNeil Consumer & Specialty Pharmaceuticals, Inc.	01 Nov 2003
Metrorrhagia	Phase 2	-	McNeil Consumer & Specialty Pharmaceuticals, Inc.	01 Nov 2003

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


AAN2019	Phase 1	-	22	Ubrogepant 50 mg	ollbyzekgz(umskhmahia) = Most (18/21) drug-related adverse events were related to ubrogepant and were mild nqtbtmvirc (otjbkwxiul ) View more	Positive	09 Apr 2019
				Ortho-Cyclen (ethinyl estradiol/norgestimate)
NCT01475513 (CTgov)	Phase 4	Cardiovascular Diseases \| Insulin Resistance	47	Ortho Cyclen® (African-American Women)	uhlwhmuquq(gwzgrcpzxc) = czlpchunlh lxyyjkfzjk (ytrfpurymy, byjkfxnmlb - wkvlqeakps) View more	-	10 Jul 2018
				Ortho Cyclen® (Caucasian Women)	uhlwhmuquq(gwzgrcpzxc) = yxuusojrfj lxyyjkfzjk (ytrfpurymy, xtaqwdpvqm - telxlaffmz) View more
NCT00775190 (CTgov)	Not Applicable	Contraception	12	ortho tricyclen (Ortho Tricyclen™)	bmkifmhjdr(bacdaumtir) = xmzwjvppit pqnjclrkij (vyyftecery, iwibgcwcvx - vvbjvhvund) View more	-	17 Apr 2017
				Trinessa (Trinessa™)	bmkifmhjdr(bacdaumtir) = jlhwjryojl pqnjclrkij (vyyftecery, zmztojiule - dgediccidj) View more
NCT01466673 (CTgov)	Phase 4	Acne Vulgaris	201	Ethinyl estradiol/Norgestimate (EE/NGM) (Ethinyl Estradiol/Norgestimate (EE/NGM))	fpyapyvezf(tpatlvdydv) = zymmectqyn fvxowwrrkf (lepicquvyg, 6.45) View more	-	19 Jun 2013
				Ethinyl estradiol+DSG+Desogestrel (Ethinyl Estradiol/Desogestrel (EE/DSG))	fpyapyvezf(tpatlvdydv) = bkbriyioge fvxowwrrkf (lepicquvyg, 7.58) View more
NCT00635570 (ACCEPT \| ClinicalTrials.gov, CTgov)	Phase 4	Contraception	273	NuvaRing (Contraceptive Vaginal Ring)	lmowmplljd = bnmmvuwnwh pmznxglfxe (wgpauyqwuu, sssfnkwads - rgrvecptsh) View more	-	07 Nov 2012
				Ortho Tri-cyclen Lo (Oral Contraceptive Pill)	lmowmplljd = fygehbketo pmznxglfxe (wgpauyqwuu, rupreerdau - hqqmhhpbdb) View more
NCT00205504 (Pubmed \| Fertil Steril)	Phase 4	-	46	combined hormonal oral contraceptive (Lean women)	lasyumiico(bjzzigmkuz) = ollxwtrlyw jsfqnzrike (kzponrahrz )	-	01 Aug 2011
				combined hormonal oral contraceptive (Obese women)	lasyumiico(bjzzigmkuz) = bygxdboxpu jsfqnzrike (kzponrahrz )