Norgestimate: A clinical overview of a new progestin

Bringer, J.

doi:10.1016/0002-9378(92)91397-s

Cited by 20 publications

(3 citation statements)

References 54 publications

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“…Norgestimate ( Figure 17 ), a steroidal oxime, (brand names, Ortho Tri-Cyclen or, Previfem, among others) is a progestin, which is used in hormonal contraception and menopausal hormone therapy for the treatment of some menopausal symptoms [ 101 ]. Norgestimate is not available as a single therapy, being used together with ethinylestradiol in birth control pills and in combination with estradiol in menopausal hormone therapy [ 102 ].…”

Section: Steroidal Oximes In Clinical Usementioning

confidence: 99%

“…Concerning the compounds in clinical trials and already in clinical use, their mechanisms are very different. Istaroxime is an inhibitor of the Na + /K + ATPase pump [ 98 ], whereas norgestimate and norelgestromin, which are already in the market for birth control, act as progesterone agonists, inhibiting ovulation [ 101 , 102 ].…”

Section: Mechanisms Of Action Of Steroidal Oximesmentioning

confidence: 99%

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The Structural Diversity and Biological Activity of Steroid Oximes

et al. 2023

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Steroids and their derivatives have been the subject of extensive research among investigators due to their wide range of pharmacological properties, in which steroidal oximes are included. Oximes are a chemical group with the general formula R1R2C=N−OH and they exist as colorless crystals and are poorly soluble in water. Oximes can be easily obtained through the condensation of aldehydes or ketones with various amine derivatives, making them a very interesting chemical group in medicinal chemistry for the design of drugs as potential treatments for several diseases. In this review, we will focus on the different biological activities displayed by steroidal oximes such as anticancer, anti-inflammatory, antibacterial, antifungal and antiviral, among others, as well as their respective mechanisms of action. An overview of the chemistry of oximes will also be reported, and several steroidal oximes that are in clinical trials or already used as drugs are described. An extensive literature search was performed on three main databases—PubMed, Web of Science, and Google Scholar.

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Section: Steroidal Oximes In Clinical Usementioning

confidence: 99%

Section: Mechanisms Of Action Of Steroidal Oximesmentioning

confidence: 99%

The Structural Diversity and Biological Activity of Steroid Oximes

et al. 2023

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“…17-desacetyl norgestimate is a metabolite of norgestimate (NGM). Norgestimate [(17R)-17-(acetyloxy)-13-ethyl-18, 19-dinor-17-pregn-4-en-20-yn-3-one oxime] is a synthetic progestational hormonal contraceptive, which regulates ovulation and menstruation [1] , [2] , [3] , [4] , [5] , [6] . Amongst the most commonly used oral contraceptives are the combination types that contain both a synthetic estrogen (ethinyl estradiol) and a synthetic progestin (norgestimate).…”

Section: Introductionmentioning

confidence: 99%

Quantification of 17-desacetyl norgestimate in human plasma by liquid chromatography–tandem mass spectrometry (LC–MS/MS) and its application to bioequivalence study

Saxena

Gupta

Kumar

et al. 2015

Journal of Pharmaceutical Analysis

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A rapid and sensitive ultra-performance liquid chromatography–tandem mass spectrometry (UPLC–MS/MS) method was developed and validated for the estimation of 17-desacetyl norgestimate in human plasma using solid-phase extraction technique. 17-desacetyl norgestimate D6 was used as the internal standard. Simple gradient chromatographic conditions and mass spectrometric detection enabled accurate and precise measurement of 17-desacetyl norgestimate at sub-picogram levels. The proposed method was validated for a linear range of 20–5000 pg/mL with a correlation coefficient ≥0.9988. The intra-run and inter-run precision and accuracy were within 10%. The overall recoveries for 17-desacetyl norgestimate and 17-desacetyl norgestimate D6 were 96.30% and 93.90%, respectively. The total run time was 4.5 min. The developed method was applied for the determination of the pharmacokinetic parameters of 17-desacetyl norgestimate following a single oral administration of a norgestimate and ethinyl estradiol 0.250 mg/0.035 mg tablets in 35 healthy female volunteers.

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