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levonorgestrel (LCS12 / LCS G04209C / MLS)

✓ Approved

Takeda · PGR · Small Molecule

What is levonorgestrel?

levonorgestrel is a small molecule developed by Takeda. It is approved for therapeutic indications via surgical implantation.

Drug Profile

Brand NamesLCS12, LCS G04209C, MLS
CompanyTakeda
Drug ClassSmall Molecule
Molecular TargetPGR
RouteSurgical Implantation
StatusApproved
Sources: ClinicalTrials.gov, Takeda

Mechanism of Action

Molecular Targets

levonorgestrel acts on 1 molecular target:

PGRprogesterone receptor (NR3C3, PR)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

levonorgestrel is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Reproductive system and breast disordersMenstrual disorder✓ Approved
Reproductive system and breast disordersHeavy menstrual bleeding✓ Approved

Related Research Articles

PubMedEpileptic disorders : international epilepsy journal with videotape2026-08-25

The effect of antiseizure medications on the exposure to combined oral contraceptives: A systematic review and network meta-analysis.

Cohen Hagar H, Mahajna Amnah Omar AO, Ben-Shushan Tomer T, Matok Ilan I et al.

Current recommendations for prescribing combined oral contraceptives (COCs) to people with epilepsy are often conflicting, particularly for weak inducers of cytochrome P450 3A4. We aimed to critically review the literature and compare the antiseizure medication (ASM)-induced changes in exposure to COC components. In this systematic review and network meta-analysis (PROSPERO: CRD42024513792), in accordance with PRISMA 2015/2020, we searched PubMed, EMBASE, Cochrane, and FDA documents up to January 2026. Eligible studies were clinical trials assessing induction (≥ 5 days) of ethinylestradiol combined with progestins by ASMs. The areas under the concentration-time curve (AUC) of individual hormones with/without the ASM were indirectly compared. The point estimate was the standardized mean difference (SMD; significant when the 95% confidence interval does not encompass zero). Bias risk was assessed using the PKclin tool. The 17 studies (16 reports) involving 399 individuals and 15 ASMs were all conducted with COCs containing the two progestins least sensitive to enzyme induction and ≥ 30 μg ethinylestradiol. Nine ASMs were studied at doses 13-75% lower than the recommended maximum (median 50%). Brivaracetam (100 mg/day) reduced the exposure to ethinylestradiol more than 1000 mg/day levetiracetam (SMD -10; 95% confidence interval - 0.20-0). The effects of 300 mg/day lamotrigine on ethinylestradiol and levonorgestrel were greater than those of 400 mg/day lacosamide (0.18; 0.11-0.25, 0.28; 0.20-0.37). Low-dose (50 mg/day) and high-dose (200 mg/day) topiramate were comparable in their effects on ethinylestradiol and norethindrone, and the low dose did not differ from weak inducers in altering ethinylestradiol exposure. Current recommendations may underestimate ASM effects on exposure to COC components, especially those in newer COCs. Greater caution is recommended with low-dose topiramate. For individuals treated with weak COC inducers without additional contraceptive means, COCs containing levonorgestrel or norethindrone might be preferable given their lower vulnerability to induction.

PMID 42640179
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PubMedContraception2026-08-24

Dynamic Patterns of LARC use in Mexico: Method mix shift between IUDs and implants and determinants of method choice.

Munduruca Stephanie S, Fuentes-Rivera Evelyn E, Trinidad Joaquin Arnoldo Escobar JAE, Schiavon Raffaela R et al.

Long-acting reversible contraceptive (LARC) methods are often grouped in contraception studies, although they differ in ways that may influence patient preferences and access. This study examines trends in IUD and implant use in Mexico, and identifies factors associated with implant use compared with IUD use. We used the 2009, 2014, 2018, and 2023 waves of the Mexican National Survey of Demographic Dynamics (ENADID). The sample included women aged 15-45 currently using LARC. We described the characteristics of LARC users in 2023 and estimated percentage point changes in prevalence for implant and IUD use as a proportion of all modern method use across survey periods. Multivariable logistic regression identified factors associated with implant use versus IUD (reference) among LARC users in 2023. The sample included 10,411 women (weighted N=4,012,772). Between 2009 and 2023, implant use increased while IUD use declined, with the largest shifts between 2018 and 2023. During this period, implant use increased by 3.48 percentage points while IUD use declined by 3 percentage points, indicating a method mix shift of implants for IUDs rather than an overall expansion of LARC use. Younger age was associated with higher odds of implant use, with odds declining with increasing age. Women with one or two children had lower odds of implant use compared with nulliparous women. Use of LARC methods in Mexico has shifted towards increased implant use and decreased IUD use, suggesting a shift between methods rather than expansion of overall LARC use. Increasing implant use alongside declining IUD use may reflect improved access but could also indicate constrained contraceptive choice. Ensuring availability of both methods is essential to support informed, patient-centered, and contraceptive decision-making.

PMID 42637068
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PubMedFood research international (Ottawa, Ont.)2026-08-24

Evaluating the potential of foodborne chemicals to modulate intestinal barrier function: a combined in vitro/in silico toolbox to study the effects on tight junction protein claudin-4.

Bergen Janice J, Fellinger Christian C, Weinstabl Magdalena M, Jobst Maximilian M et al.

Intestinal barrier integrity is of paramount importance for our health. Several food constituents and contaminants have been described for positive or detrimental effects, however, a correlation between gut associated disorders and xenobiotics exposures remains challenging and modeling options limited. This study presents a NAMs-based hybrid in vitro/in silico workflow to investigate, and eventually prioritize, foodborne xenobiotics for their effect on gut barrier homeostasis. Model compounds comprised endocrine-active chemicals, such as plastic components (bisphenol A, bisphenol F), phytoestrogens (chrysin, daidzein, genistein), mycotoxins (alternariol, zearalenone), and natural/synthetic steroids (17-β-estradiol, cholesterol, levonorgestrel). Plasticizer diisodecyl phthalate was included as foodborne, non-endocrine active substance. The Caco-2/HT29-MTX-E12 intestinal epithelial co-culture was used to design a workflow capable of grasping discrete alterations in tight junction organization. The protein claudin-4 was taken as reference to study the structural organization along cell-cell contacts. Complementarily, docking and molecular dynamics simulations were applied to explore ligand-claudin-4 interactions, providing a pipeline which is potentially suitable to screen larger compounds libraries. Finally, proof-of-principle experiments including repeated exposures to reference compound 17-β-estradiol and plasticizer diisodecyl phthalate, supported the plausibility of a functional impairment of claudin-4. Both compounds significantly increased epithelial permeability without altering cell viability, indicating selective modulation of mechanical barrier properties. Together, this work outlines a mechanistic toolbox for the study of the potential of orally derived xenobiotics in modulating intestinal homeostasis.

PMID 42637315
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PubMedJournal of obstetrics and gynaecology of India2026-08-22

Analysis of Non-responders to LNG-IUS in Cases of Heavy Menstrual Bleeding.

Savani Gayatri G, Kumari Saroj S, Ravinarayan Shruti S, Mishra Nigamananda N

Heavy menstrual bleeding (HMB) or menorrhagia, a common complaint among women during their reproductive years, significantly impacts women's quality of life, productivity, and healthcare costs. The treatment options range from conservative medical management to minimally invasive procedures and hysterectomy. While levonorgestrel-intrauterine system (LNG-IUS) is established as an effective treatment for HMB, there is a lack of significant research on factors determining non-response in women with HMB. This study aims to analyse the factors behind non-response to LNG-IUS in women with HMB. A retrospective observational study was conducted at BARC Hospital, Mumbai, from January 2017 to March 2020, including 88 patients with HMB who received LNG-IUS. Non-responders to LNG-IUS were analysed for reasons of failure, including endometrial thickness, hysteroscopy, and biopsy reports. Patients were contacted one year later to assess treatment outcomes, and alternative treatments or surgery was offered to non-responders, with final histopathological findings documented. In this study, 29.5% of patients were non-responders, with the majority aged 40-44 years, and most experiencing persistent heavy bleeding, dysmenorrhea, device expulsion, or misplacement. Half of the non-responders had an endometrial thickness of less than 10 mm and proliferative endometrium on biopsy. Nine patients underwent hysterectomy, with adenomyosis found in seven of them. LNG-IUS is effective in treating HMB, but factors, such as age, endometrial thickness, and certain underlying structural and non-structural pathologies, may contribute to non-response.

PMID 42630355
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PubMedContraception2026-08-21

Twelve-Month Outcomes of Rotated Copper Intrauterine Devices After Immediate Postpartum Insertion.

Castro Thais Bezerra Vasconcelos de TBV, Nóbrega Aureliana Barboza da Silva ABDS, Coutinho Conrado Milani CM, Vieira Carolina Sales CS

To describe clinical outcomes of copper intrauterine devices (Cu-IUDs) inserted immediately postpartum that subsequently assumed a rotated position. Secondary analysis of a postpartum IUD cohort using medical record data from women with rotated Cu T380A IUDs identified by transvaginal ultrasound 30-120 days after delivery who elected to maintain the device and were followed for 12 months. Among 2,105 insertions, 1,813 had follow-up data available. Ninety-three devices (5.1%) were rotated. Of these, 73 asymptomatic women elected to maintain the device and were followed for 12 months. Partial uterine perforation occurred in 24 (32.9%), partial expulsion in 2 (2.7%), and no pregnancies were observed. Overall, 35 women (47.9%) discontinued use, primarily due to perforation. Rotated postpartum Cu-IUDs were not associated with pregnancy and rarely expelled but frequently progressed to partial uterine perforation.

PMID 42628711
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PubMedContraception2026-08-20

Risk of ischemic and hemorrhagic stroke in users of progestogen-only contraceptives: A Danish registry study.

Letnar Gasper G, Andersen Klaus Kaae KK, Olsen Tom Skyhøj TS

We studied the risk of ischemic (IS) and hemorrhagic stroke (ICH) in users of progestogen-only contraceptives (POCs): levonorgestrel-releasing intrauterine device (LNG-IUD), progestogen-only pill (POP), implant and injection. In this nationwide cohort study using Danish registry data for all women aged 18-49 years, 2004-2021, we estimated incidence rate ratios (IRRs) for IS and ICH associated with POC use. Comparisons were made with non-use of hormonal contraception and with combined hormonal contraceptives (CHC) with ethinylestradiol containing equivalent progestogens. Poisson regression models were adjusted for age, ethnicity, education, calendar year, and risk factors. A total of 1,734,905 non-pregnant women contributed 16,854,953 person-years of follow-up. The most frequently used POCs were LNG-IUD (1,720,931 person-years), followed by desogestrel-only pills (255,404), norethisterone-only pills (104,261), etonogestrel implants (61,756), and medroxyprogesterone injections (27,469). CHCs with ethinylestradiol accounted for 4,431,841 person-years. Compared with non-use of hormonal contraception, no POC type was associated with increased adjusted IRRs for IS or ICH. Compared with CHCs containing desogestrel or levonorgestrel in addition to ethinylestradiol, adjusted IRRs for IS were significantly lower for desogestrel-only pills (IRR 0.56, 95%CI 0.38, 0.82) and LNG-IUD (IRR 0.44, 95%CI 0.36, 0.53). IRRs for ICH were not significantly changed: LNG-IUD 0.85 (95%CI 0.37, 1,92); desogestrel-only pills 0.98 (95%CI 0.44, 2,20). POCs were not associated with increased stroke risk. Relative to CHCs with ethinylestradiol, POCs were linked to approximately half the risk of IS. However, the absolute number of strokes avoided by choosing POCs over CHCs with ethinylestradiol is small and, for most women-particularly those under 40 years-unlikely to be clinically detectable. POCs-including POPs, implants, injections, and LNG-IUDs-were not associated with an increased risk of either IS or ICH and support their use as appropriate alternatives to CHCs with ethinylestradiol for women in whom stroke risk is an important clinical consideration.

PMID 42624314
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