High inhibition ratio and transformation index of 2 mg dienogest: further evidence for its use in endometriosis treatment

Pedro Viana Pinto, Pinto PV, Barretta M, Marta Barretta, Giovanni Grandi, Grandi G
The European journal of contraception & reproductive health care : the official journal of the European Society of Contraception · 2025 · vol. 31(1) , pp. 48–52 · doi:10.1080/13625187.2025.2589998 · PMID:41329046 · W4416915328
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Dienogest at 2 mg/day demonstrates a high transformation index and inhibition ratio, reinforcing its unique properties and suitability for endometriosis treatment.

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This review examines the pharmacological profile of dienogest, a fourth-generation progestin approved for treating endometriosis. It highlights recent metrics such as the inhibition ratio and transformation index, noting that a 2 mg daily dose yields a transformation index of approximately 933% and a cyclical inhibition ratio of 200%. These specific properties distinguish dienogest from other progestins, reinforcing its efficacy in managing pain and preventing lesion recurrence across various forms of the disease. This paper is centrally about endometriosis — specifically evaluating the unique pharmacological advantages of dienogest for its treatment.

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Abstract

Endometriosis is a common, chronic disease with a high burden for women, characterised by the implantation of endometrial cells outside the uterus. Many different treatments have been proposed for this disease, mainly hormonal, with the objective of inducing amenorrhoea and a hypoestrogenic environment. Dienogest (DNG), a fourth-generation progestin, has received approval for the treatment of endometriosis in many countries. Its pharmacological properties make it especially attractive for the treatment of this disease. Several trials demonstrated the clinical efficacy in managing endometriosis-associated pain, preventing symptoms, and reducing lesion recurrence. Its efficacy has been proven both for deep infiltrative endometriosis and ovarian endometriosis, and its long-term safety and tolerability are also well established. Recently, the inhibition ratio and the transformation index for progestins have been proposed. DNG at the used dose of 2 mg/daily, with a transformation index of around 933% and a cyclical inhibition ratio of 200%, appears to have very specific progestin properties, unique among different molecules of the same groups, reinforcing its leading role in the treatment of endometriosis.
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Abstract Endometriosis is a common, chronic disease with a high burden for women, characterised by the implantation of endometrial cells outside the uterus. Many different treatments have been proposed for this disease, mainly hormonal, with the objective of inducing amenorrhoea and a hypoestrogenic environment. Dienogest (DNG), a fourth-generation progestin, has received approval for the treatment of endometriosis in many countries. Its pharmacological properties make it especially attractive for the treatment of this disease. Several trials demonstrated the clinical efficacy in managing endometriosis-associated pain, preventing symptoms, and reducing lesion recurrence. Its efficacy has been proven both for deep infiltrative endometriosis and ovarian endometriosis, and its long-term safety and tolerability are also well established. Recently, the inhibition ratio and the transformation index for progestins have been proposed. DNG at the used dose of 2 mg/daily, with a transformation index of around 933% and a cyclical inhibition ratio of 200%, appears to have very specific progestin properties, unique among different molecules of the same groups, reinforcing its leading role in the treatment of endometriosis. SHORT CONDENSATION Dienogest has particular properties that make it an attractive option for the treatment of endometriosis. The newly described inhibition ratio and transformation index for progestins reinforce its position among progestins for the treatment of endometriosis. 摘要 子宫内膜异位症是一种常见的慢性疾病, 对女性健康构成显著负担, 其特征为子宫内膜细胞在子宫外异常种植。目前该病的治疗方案多样, 主要采用激素疗法, 旨在诱导闭经并建立低雌激素状态。地诺孕素作为一种第四代孕激素, 已在多国获准用于子宫内膜异位症治疗。其药理学特性使其在该病治疗中具有独特优势。多项临床研究证实, 地诺孕素能有效控制子宫内膜异位症相关疼痛、预防症状发作并降低病灶复发率, 无论在深部浸润型或卵巢型子宫内膜异位症中均显示出明确疗效, 且长期应用安全性与耐受性良好。近期研究提出以抑制率与转化指数评估孕激素活性。地诺孕素在2mg/日的常规剂量下, 转化指数约达933%, 周期性抑制率高达200%, 表现出特异性的孕激素活性, 在同类别药物中独具优势, 进一步奠定了其在子宫内膜异位症治疗中的重要地位。 Disclosure statement No potential conflict of interest was reported by the author(s).

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Condition tags

endometriosis

MeSH descriptors

Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis

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