The paradigm of norgestimate: a third-generation testosterone-derivative progestin with a peripheral anti-androgenic activity and the lowest risk of venous thromboembolism.
Expert Rev Clin Pharmacol
; 14(2): 211-224, 2021 Feb.
Article
in En
| MEDLINE
| ID: mdl-33464138
ABSTRACT
INTRODUCTION:
Norgestimate (NGM) is a testosterone derivative with peculiar receptor activities. AREAS COVERED This is a narrative review of the available data on the pharmacotherapy of NGM in combined hormonal contraceptives (CHCs) in terms of contraceptive efficacy, venous thromboembolism (VTE) risk, safety, tolerability and bleeding patterns. A comprehensive literature review was conducted in August 2020 using PubMed with the keyword 'norgestimate'. EXPERT OPINION NGM shows a mild estrogenic activity associated with anti-mineralocorticoid and anti-androgenic properties, largely responsible for the cardiovascular safety profile. The anti-androgenic property depends on the androgen receptor (AR) nuclear translocation (AR trafficking and its subnuclear distribution), the inhibition of 5α-reductase activity (it possesses higher activity compared to other available progestins), and the increase on sexual hormone binding globulin (SHBG) levels if combined with an estrogenic counterpart. NGM is one of the molecules that best modulates the power of ethinyl-estradiol on the thromboembolic risk, being associated with the lowest VTE risk between different CHCs. NGM has the advantage of retaining peripheral anti-androgenic activity, demonstrated by the impact on lipid and glucose metabolism, and it should be preferred if compared with other similar progestins of the same class of risk which are much more androgenic, such as levonorgestrel.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Venous Thromboembolism
/
Contraceptive Agents, Hormonal
/
Norgestrel
Type of study:
Etiology_studies
/
Risk_factors_studies
Limits:
Animals
/
Female
/
Humans
Language:
En
Journal:
Expert Rev Clin Pharmacol
Year:
2021
Document type:
Article
Affiliation country:
Italia