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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

Mechanism of Action

Molecular Targets

levonorgestrel acts on 1 molecular target:

PGRprogesterone receptor (NR3C3, PR)
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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

PubMedRadiographics : a review publication of the Radiological Society of North America, Inc2026-10-15

Updated Terminology for Multidisciplinary Management of Intrauterine Devices: A Proposed Lexicon.

Jones Jill A JA, Boatright Christine M CM, Williams Vanessa L VL, Keller Jessica J JJ et al.

There are numerous terms used to describe variant locations of intrauterine devices (IUDs) in US reports, such as displaced, low lying, and malpositioned. These vague terms are frequently misinterpreted by providers and patients, which may lead to an incorrect inference of inadequate contraception. Current consensus guidelines from the American College of Obstetricians and Gynecologists (ACOG) indicate that the greatest risk of unintended pregnancy may be due to the unnecessary removal of a nonfundal IUD. Many providers now advocate leaving an IUD in place if it is located entirely above the internal os, as the device still provides effective contraception. The ACOG recommends counseling for patients, whether symptomatic or asymptomatic, before removal of the IUD. The authors outline a simple lexicon to describe the location of IUDs in US reports that includes terms understood by obstetrics and gynecology providers and that better align with current gynecologic literature. ©RSNA, 2026 Supplemental material is available for this article.

PubMedBJOG : an international journal of obstetrics and gynaecology2026-10-15

Efficacy and Safety of Lidocaine Compared to Other Agents for Intrauterine Device Insertion Pain: A Systematic Review and Meta-Analysis.

Pirrami Rachael G RG, Pandya Greeshma G, Islam Aminah A, Shaw Jalyn J et al.

Pain during intrauterine device (IUD) insertion remains a common barrier to use, with limited guidance on preferred pharmacological agents. Evaluate the efficacy and safety of lidocaine compared to other pharmacologic agents for reducing pain during IUD insertion. Electronic database searches were conducted in August 2025 and included randomized controlled trials (RCTs) published between January 1984 and August 2025. RCTs involving women or adolescents that evaluated the efficacy and safety of lidocaine versus other pharmacologic agents for reducing IUD insertion pain. Conducted in accordance with Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) methodology. Risk of bias was assessed using the Cochrane Risk of Bias Tool for Randomized Trials (RoB-2) and meta-analysis was conducted on 5 of the 6 studies using Meta-Analysis version 4.0.2. Six studies (N = 658) compared lidocaine to non-steroidal anti-inflammatory drugs (NSAIDs) or misoprostol. Of these, two studies showed statistically significant pain reduction with lidocaine versus NSAIDs (study 1: 5.4 ± 2.8 vs. 7.3 ± 2.1, p < 0.001; study 2: 2.6 ± 0.9 vs. 4.1 ± 1.1, p < 0.001). The meta-analysis showed no statistically significant pain reduction with lidocaine overall. Lidocaine did not demonstrate a statistically significant reduction in pain. It remains unclear whether lidocaine, NSAIDs, and misoprostol are clinically comparable options. Secondary outcomes varied, and safety data were limited, highlighting the need for standardized endpoints. Further head-to-head trials are needed to guide optimal pain management for IUD insertion.

PubMedNeuropharmacology2026-10-15

N-acetylcysteine decreases toluene conditioned place preference and modulates corticostriatal activity in adolescent rats.

Carampel Ajina C AC, Asis Joannes Luke B JLB, Munar Johanna C JC, Gregorio Cynthia Grace C CGC et al.

Inhalant (toluene) use disorder (IUD) continues to be a public health problem especially among Filipino adolescents. Animal models of IUD have not explored neurobiological changes from chronic toluene exposure, or possible treatments for long-lasting toluene-induced deficits. In rats repeatedly exposed to 3000 ppm of toluene vapor over 12 days, we report that daily administration of N-acetylcysteine (NAC; 100 mg/kg i.p. or 0.9 g/l oral), but not melatonin (10 mg/kg i.p.), during 8 days of abstinence reduced toluene conditioned place preference in both male and female adolescent Sprague-Dawley rats. Using immunofluorescence, we found that toluene-exposed rats showed decreased c-Fos densities in the dorsomedial striatum (DMS), dorsolateral striatum, and ventrolateral orbitofrontal cortex (vlOFC) after 8 days of abstinence. NAC partially rescued c-Fos expression in vlOFC. We found that c-Fos densities in both vlOFC and prelimbic cortex were significantly correlated with CPP values and with c-Fos densities in the DMS across treatment groups, suggesting that a history of toluene exposure may act by reducing cortical modulation of the dorsal striatum to promote long-lasting drug context-seeking. Our findings suggest that N-acetylcysteine may be a promising treatment for IUD in adolescent males and females.

PubMedBMC psychiatry2026-10-15

Epigenetics of generalized internet use disorder including data on overuse of social media: a closer look at the SLC6A4, NR3C1 and OXT genes.

Montag Christian C, Kiefer Markus M, Connemann Bernhard J BJ, Kammer Thomas T et al.

Only few studies so far have investigated the molecular underpinnings of Internet Use Disorders (IUD), which can shed light on the neurochemical basis of excessive online behaviors. There are even less epigenetic studies in this research field, and longitudinal evidence is even more scarce. The present study investigated in n = 83 depressed patients and n = 83 healthy controls potential links between DNA-methylation of three candidate genes (serotonin transporter gene SLC6A4, glucocorticoid receptor gene NR3C1 and gene coding for oxytocin OXT) known to play a role in affective disorders and self-reported excessive Internet and problematic social media use over a two-week period. In depressed patients, we found a significant positive association between problematic social media use, IUD tendencies in general, craving and methylation of a CpG site in NR3C1. In healthy controls, we found a significant positive association between social support and methylation of a CpG site in OXT. Further we found that higher social media addiction tendencies were associated with decreasing differences in methylation of OXT over a two-week period in both the group of depressed patients and healthy controls. However, this effect was small and the confidence interval contained zero. Our findings might provide first preliminary indications that NR3C1 and OXT might be involved in overuse of social media. However, small effect sizes and complex interaction effects require replication in larger samples with longitudinal measurements over a longer time period.

PubMedOpen medicine (Warsaw, Poland)2026-10-13

Hysteroscopic polypectomy with vs. without levonorgestrel-releasing intrauterine system in women with endometrial polyps and dysmenorrhea.

Ni Yongyan Y, Chen Yue Y

To evaluate, among premenopausal women with endometrial polyps and documented dysmenorrhea, whether levonorgestrel-releasing intrauterine system (LNG-IUS) placement after hysteroscopic polypectomy (HP) was associated with better outcomes. This retrospective cohort study analyzed 276 premenopausal women with pathologically confirmed endometrial polyps who underwent HP between January 2022 and December 2024. Patients were classified into an HP-alone group (n=162) or an HP+LNG-IUS group (n=114). At 12 months, the HP+LNG-IUS group had lower VAS scores than the HP group (aMD=-0.36; 95 % CI, -0.60 to -0.12; p=0.004). Clinically meaningful dysmenorrhea improvement occurred in 79.82 % in the HP+LNG-IUS group and 65.43 % in the HP group (aOR, 2.22; 95 % CI, 1.23-3.99; p=0.008). HP+LNG-IUS was also associated with a lower 12-month PBAC score and thinner endometrium. Exploratory analyses showed lower measured FSH, LH, estradiol, and progesterone levels. Polyp recurrence was observed in 2.63 % in the HP+LNG-IUS group and 9.26 % in the HP group. In this study, LNG-IUS placement after HP was associated with modestly lower pain scores, lower menstrual blood loss, thinner endometrium, and lower observed 12-month polyp recurrence. Residual confounding, sparse recurrence events, ultrasound-based recurrence ascertainment, and retrospective adverse-event capture limit causal and safety inferences. Prospective controlled studies are required.

PubMedIntegrated environmental assessment and management2026-10-13

THE Environmental Impact of Contraceptive Methods - A Systematic Review.

van der Heide E E R EER, Cohen E S ES, Pieters L I LI, van Heel D A M DAM et al.

Contraception contributes to healthcare's global environmental footprint through pharmaceutical emissions and disposable waste. Steroid hormones used in hormonal contraception are widely detected in aquatic environments, raising concerns regarding their ecotoxicological risks. This review synthesizes environmental impacts of registered (non-)hormonal contraceptives, aiming to compare their environmental sustainability and estimate comparative ecotoxicological risk profiles of hormonal methods. A systematic literature search of Medline, Embase, Web of Science Core Collection, and Scopus was conducted through January 8, 2026, covering life cycle assessments, carbon footprint studies, water monitoring studies, chronic ecotoxicological effect studies, and environmental risk assessments. Of 3,409 records retrieved, 78 studies met predefined inclusion criteria. Extracted data were organised by study type, contraceptive method, environmental impact categories, and ecotoxicological endpoints. Available life cycle assessments were limited to condoms and showed that natural rubber condoms were associated with lower production-related environmental burden than polyisoprene condoms. The total waste associated with the use of long-acting hormonal contraceptives was lower compared to short-acting methods and non-hormonal intrauterine devices. Environmental risk assessments revealed global occurrence of estrogens and progestins in surface waters, with some posing risks to aquatic ecosystems. Comparative ecotoxicological profiles suggested lower relative ecotoxicity for drospirenone- and desogestrel-containing oral contraceptives per daily dose compared with other hormonal methods, and potentially lower ecotoxicity for levonorgestrel intrauterine devices compared to levonorgestrel containing oral formulations. Overall, the included studies reported on only a limited range of environmental impacts, such as waste production, carbon footprint and ecotoxicity, while overlooking other aspects of environmental sustainability. Because of this no definitive conclusions or comparisons could be made based on the full environmental sustainability. However, by extending the focus beyond direct environmental impacts towards overall sustainability, different contraceptive groups were ranked according to their overall sustainability. This led to the conclusion that long-acting reversible contraceptives are relatively more sustainable then short-acting reversible methods.

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