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drospirenone (Slinda / LPRICF113 / LF111)

✓ Approved

HyundaiPharm · ESR1 · Steroids

What is drospirenone?

drospirenone is a steroids developed by HyundaiPharm. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesSlinda, LPRICF113, LF111
CompanyHyundaiPharm
Drug ClassSteroids, Small Molecule
Molecular TargetESR1, ESR2, NR3C2, PGR
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, HyundaiPharm

Mechanism of Action

Molecular Targets

drospirenone acts on 4 molecular targets:

ESR1estrogen receptor 1 (ER, ESR)
ESR2estrogen receptor 2 (ESTRB, ER-BETA)
NR3C2nuclear receptor subfamily 3 group C member 2 (NR3C2VIT, MR)
PGRprogesterone receptor (NR3C3, PR)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

drospirenone is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Reproductive system and breast disordersDysmenorrhoeaPhase II

Related Research Articles

PubMedResearch and practice in thrombosis and haemostasis2026-08-28

Effects of estetrol/drospirenone vs drospirenone-only on thrombin generation in women with polycystic ovary syndrome: a randomized, double-blind, controlled trial.

Chantrapanichkul Panicha P, Wiwatboworn Paveenutch P, Rattanachaiyanont Manee M, Tanmahasamut Prasong P et al.

Combined oral contraceptives are first-line treatment for polycystic ovary syndrome (PCOS); however, venous thromboembolism risk remains a concern. Estetrol/drospirenone (E4/DRSP) has a more favorable thrombin generation assay (TGA) profile than ethinyl estradiol-based combined oral contraceptives, but direct comparison with progestin-only pills is lacking. This study aimed to compare the effects of E4/DRSP and DRSP-only on TGA parameters, hyperandrogenic symptoms, and vaginal bleeding patterns in women with PCOS. In a randomized, double-blind, controlled trial, women with PCOS aged 18 to 40 years at Siriraj Hospital, Thailand (May-December 2025) were assigned in a 1:1 ratio to E4/DRSP or DRSP-only for 12 weeks. The primary outcome was change in TGA parameters measured with and without thrombomodulin (TM). Secondary outcomes were vaginal bleeding patterns, modified Ferriman-Gallwey score, acne severity, and treatment satisfaction. Both regimens increased endogenous thrombin potential and peak height on TGA, without TM (E4/DRSP: 1699 to 1888; DRSP-only: 1836 to 2085 nM·min; within-group P ≤ .017) and with TM (both P = .001), with no between-group differences (all P > .05). The endogenous thrombin potential-TM ratio rose in both groups, with no between-group difference (E4/DRSP: median +0.14; DRSP-only: +0.13; between-group P = .74). DRSP-only had fewer scheduled bleeding days across 3 cycles, whereas E4/DRSP reduced modified Ferriman-Gallwey score for hirsutism (P < .001). Waist-to-hip ratio, acne, and treatment satisfaction were comparable, with no serious adverse events. E4/DRSP and DRSP-only had comparable effects on thrombin generation and TM-mediated anticoagulation in women with PCOS. E4/DRSP reduced hirsutism, supporting its consideration as a treatment option for PCOS.

PMID 42662895
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PubMedJournal of computer-aided molecular design2026-08-26

In silico discovery of RIOK3 inhibitors against pancreatic ductal adenocarcinoma using homology modelling, molecular docking, molecular dynamics simulations, ADMET prediction, and MTT assay.

Alhussieni Kawthar K, Othman Rozana R, Thamaraikani Tamilanban T, Tan Ke Han KH et al.

Pancreatic ductal adenocarcinoma (PDAC) is an aggressive cancer strongly linked to RIO Kinase 3 (RIOK3), which promotes progression by stabilizing and phosphorylating Focal Adhesion Kinase (FAK). Advances in protein structure prediction, particularly AlphaFold2, have significantly enhanced our understanding of protein dynamics, aiding in the identification of potential inhibitors for targeted therapies. This study used structure-based virtual screening, molecular dynamics simulations, ADMET/toxicity prediction, and in vitro validation to identify potential inhibitors of RIOK3 for PDAC treatment. The 3D structure of RIOK3 was predicted using AlphaFold2 and docked with compounds listed in the ZINC database that were independently confirmed as FDA-approved drugs using AutoDock Vina. Pharmacokinetic and pharmacodynamic properties were assessed with SwissADME, and in vitro validation was performed using MTT assays to assess cell viability and growth inhibition. Four top-scoring compounds were identified, with binding energies between - 11.3 and - 10.4 kcal/mol. Venetoclax showed the most stable complex with RIOK3, followed by Conivaptan and Irinotecan. Drospirenone showed weaker binding. Molecular dynamics simulations and MM/GBSA analysis supported the stability of these complexes. SwissADME and ProTox-II confirmed that the compounds met drug-likeness criteria but exhibited distinct pharmacokinetic and toxicity profiles. In vitro MTT assays showed concentration-dependent growth inhibition in PANC-1 cells, with Venetoclax having the lowest IC₅₀ value. This study identifies RIOK3 as a promising therapeutic target for PDAC, with Venetoclax, Conivaptan, Drospirenone, and Irinotecan as repurposable candidates for further research. Further studies should include biochemical assays, expanded cytotoxicity profiling in multiple PDAC cell lines, and in vivo evaluations to validate RIOK3-targeted therapies for PDAC treatment.

PMID 42645594
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PubMedFrontiers in endocrinology2026-08-08

Estetrol/drospirenone for combined oral contraception: a systematic review of efficacy, cycle control, and safety.

Sánchez-Prieto Manuel M, Coll Sandra S, Romero-Domínguez Marina M, Avella-Marcos Marta M et al.

To systematically evaluate the evidence on the contraceptive efficacy, cycle control, safety, and selected noncontraceptive effects of estetrol 15 mg/drospirenone 3 mg (E4/DRSP) and to assess certainty of evidence by outcome using the GRADE approach. A systematic review was conducted in accordance with PRISMA 2020. PubMed/MEDLINE, Scopus, and Google Scholar were searched for eligible studies published through February 2026. Clinical trials and comparative studies evaluating E4/DRSP in women of reproductive age were included. Outcomes were grouped into contraceptive efficacy, bleeding/cycle control, safety and tolerability, hemostatic and endocrine-metabolic effects, ovarian suppression, and noncontraceptive clinical outcomes. Risk of bias was assessed using design-specific tools, and certainty of evidence was graded by outcome. A total of 25 eligible publications/study reports were included, comprising phase 2 dose-finding studies, pivotal phase 3 contraceptive trials, pooled analyses, mechanistic comparator studies, adolescent data, and indication-specific studies. E4/DRSP demonstrated robust contraceptive efficacy, predictable bleeding patterns, and an acceptable tolerability profile. Across mechanistic studies, E4/DRSP showed less pronounced hemostatic and endocrine-metabolic effects than ethinyl estradiol-containing comparators. The most consistent biological differentiation of E4/DRSP was observed for APC resistance and thrombin-generation endpoints, which were less affected than with EE-containing comparators. The strongest noncontraceptive evidence was observed for dysmenorrhea, supported by a randomized, double-blind, placebo-controlled trial. Certainty of evidence was moderate for contraceptive efficacy, cycle control, common adverse events, and surrogate hemostatic/metabolic outcomes; high for dysmenorrhea versus placebo; low for endometriosis-related and menstrual symptom outcomes; and very low for clinical thromboembolic risk. E4/DRSP is an effective combined oral contraceptive with favorable cycle control and a consistent biologic profile suggesting lower hepatic/hemostatic impact than ethinyl estradiol-containing formulations. However, current evidence does not establish comparative thromboembolic safety, which requires dedicated postauthorization and real-world comparative studies.

PMID 42568434
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PubMedRevista brasileira de ginecologia e obstetricia : revista da Federacao Brasileira das Sociedades de Ginecologia e Obstetricia2026-07-25

Hemostatic safety profile of estetrol vs. ethinylestradiol in oral contraceptives: a systematic review and meta-analysis.

Lemos Maria Julia MJ, Ferraz Jacqueline Maia JM, Queiroz Laura Fonseca LF, Diniz Alice França AF et al.

To evaluate the hemostatic profile of estetrol/drospirenone (E4/DRSP) compared with ethinylestradiol/drospirenone (EE/DRSP) in adult women. A systematic review and meta-analysis of randomized controlled trials (RCTs) was performed according to PRISMA guidelines. Eligible studies compared E4/DRSP with EE/DRSP in adult women and assessed coagulation, anticoagulation, or fibrinolytic markers. Three RCTs (n=183) met inclusion criteria. Data were extracted independently, and pooled mean differences (MD) were calculated using random-effects models. Compared to EE/DRSP, E4/DRSP was associated with higher protein S activity (MD = 21.23; 95% CI: 11.83 to 30.64; p<0.00001) and lower levels of fibrinogen (MD = -24.17; 95% CI: -39.15 to -9.19; p=0.002), plasminogen (MD = -27.28; 95% CI: -27.28 to - 22.89; p<0.00001), and SHBG (MD = -183.38; 95% CI: -183.38; 95% CI: -210.93 to -155.84; p<0.00001). No significant differences were observed for D-dimer and antithrombin. Protein C activity was higher in the EE group, though this was an isolated finding with limited interpretability. E4/DRSP demonstrates a more favorable hemostatic profile than EE/DRSP, potentially reducing thrombotic risk. Despite the limited number of RCTs, consistency across markers supports E4 as a safer estrogenic component for contraceptive formulations, with implications for women at increased risk of venous thromboembolism.PROSPERO registry: #CRD420251074961.

PMID 42500171
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PubMedInternal medicine journal2026-07-12

Tolerability of hormonal treatments in acute hepatic porphyria patients.

Arandjelovic Andjela A, Ross Charlotte C, Ross Gayle G

Acute hepatic porphyria (AHP) flares have been associated with female hormones and the use of hormonal treatments. Women with AHP are traditionally advised to avoid exogenous oestrogen and progesterone, limiting options for contraception and management of menorrhagia, dysmenorrhoea and menopausal symptoms. Evidence on specific hormonal therapies is limited; a 2003 study found that 25% of women with acute intermittent porphyria (AIP) experienced attacks with contraceptives containing progesterone, oestrogen or both. To update the current understanding of the tolerability of hormonal treatments in women with AHP. An anonymous questionnaire was distributed to women with AHP (acute intermittent porphyria, hereditary coproporphyria and variegate porphyria) via hospital records and a national patient support group, capturing prior hormonal therapy use and associated flares. Thirty responses were analysed; 23 participants had used hormonal therapies. Flares were most frequent in hereditary coproporphyria (66%) and less common in variegate porphyria and acute intermittent porphyria (~20%). No flares were reported with hormone replacement therapy, the progesterone-only pill or progesterone implants. Flares occurred with combined oral contraceptives (46.6%) and progesterone-containing intrauterine devices (28.5%), particularly drospirenone-containing pills. Levonorgestrel-based therapies, including the Mirena IUD, were better tolerated and often improved symptoms. Although limited by sample size and retrospective design, this study provides clinically useful data on the tolerability of specific hormonal therapies in women with AHP, supporting personalised prescribing and patient counselling for contraception and symptom management.

PMID 42435415
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PubMedHypertension research : official journal of the Japanese Society of Hypertension2026-07-08

Oral contraceptive-associated hypertension as an under-recognized contributor to secondary and apparent resistant hypertension: agent-specific blood pressure liability, RAAS testing pitfalls, and practical assessment.

Furuto Yoshitaka Y, Yoshino Daiki D, Namikawa Akio A, Sato Dai D et al.

Oral contraceptive-associated hypertension is a long-recognized yet still under-recognized and potentially reversible contributor to elevated blood pressure in women, particularly adolescents and young adults. In Japan, prescribing of low-dose estrogen-progestin preparations has increased; however, available prescription data neither demonstrate an increase in oral contraceptive-associated hypertension nor establish a pill-specific rise in blood pressure among young women. Hormonal exposure may be overlooked because patients may not identify hormonal pills as blood pressure-relevant medicines and because contraceptive prescribing and hypertension assessment often occur in separate clinical settings. Oral contraceptive use may contribute to new-onset hypertension, worsening of established hypertension, apparent resistant hypertension, and misinterpretation of renin-angiotensin-aldosterone system testing. Blood pressure liability varies by formulation: ethinyl estradiol-containing combined hormonal contraceptives warrant the greatest concern, whereas drospirenone-containing or estradiol-based combined pills, progestin-only pills, and implants generally have lower or more neutral blood pressure signals. This review integrates targeted exposure recognition, formulation-specific assessment, home and ambulatory blood pressure monitoring, practical interpretation of a mildly elevated aldosterone-to-renin ratio, and coordinated management of women with new, worsening, or apparent resistant hypertension.

PMID 42414602
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