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levonorgestrel (LCS12 / LCS G04209C / MLS)

✓ Approved

Takeda · PGR · 小分子

什么是 levonorgestrel?

levonorgestrel 是一种小分子,由Takeda研发。该药已获批,用于治疗相关适应症,给药途径:Surgical Implantation。

药物档案

商品名LCS12, LCS G04209C, MLS
公司Takeda
药物类别小分子
分子靶点PGR
给药途径Surgical Implantation
状态Approved

作用机制

分子靶点

levonorgestrel 作用于 1 个分子靶点:

PGRprogesterone receptor (NR3C3, PR)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

levonorgestrel 针对 2 个适应症,涉及 1 个治疗领域。

治疗领域疾病/病症分期
Reproductive system and breast disordersMenstrual disorder✓ Approved
Reproductive system and breast disordersHeavy menstrual bleeding✓ Approved

相关研究文献

PubMedRadiology case reports2026-10-25

Urologically silent intravesical migration of a copper intrauterine device presenting as chronic pelvic pain: CT features and comparison with reported cases.

Hafsi Montacer M, Zouaghi Asma A, Yaich Oumayma O, Hafsi Azer A et al.

Uterine perforation with migration of an intrauterine device (IUD) into the urinary bladder is a well-documented complication that usually presents with lower urinary tract symptoms, recurrent urinary tract infection, hematuria, or a secondary bladder calculus. We report a 35-year-old woman (G2P2) with a copper IUD inserted 5 years earlier who presented with progressive chronic pelvic pain and no urinary symptoms. Pelvic ultrasound showed an abnormally positioned device, and contrast-enhanced computed tomography (CT) demonstrated a T-shaped device of metallic density traversing the anterior uterine wall, with one arm protruding into the bladder dome and coated by a small encrustation. The fixed, non-dependent position of the linear metallic core, its continuity with the myometrium, and its T-shaped morphology distinguished the device from a primary bladder calculus. Cystoscopy confirmed partial intravesical protrusion of the encrusted arm, which was extracted intact with forceps without complication, and the patient was asymptomatic at follow-up. Compared with published intravesical cases, in which urinary complaints or a bladder stone usually prompt investigation, this case shows that bladder involvement may remain silent from a urinary perspective. In IUD users with unexplained pelvic pain, imaging should specifically assess the bladder, and a delayed excretory CT phase is advisable to evaluate bladder-wall integrity before removal.

PMID 42921231
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PubMedAmerican journal of obstetrics and gynecology2026-10-25

Assessing the Safety of Estro-Progestin and Progestin-only drugs: A Signal Detection Study of Meningioma Reports in EudraVigilance.

Manuzzi Alice A, Fazio Elena E, Nikitina Victoria V, Broccoli Massimiliano M et al.

Exogenous hormonal therapies are used for contraception and for several gynecologic and menopausal indications, frequently for prolonged periods. Previous epidemiological studies have reported an increased risk of meningioma with some progestins, particularly following prolonged exposure and high cumulative doses. It is a common intracranial tumor with marked female predominance, suggesting a potential role of hormones in its pathogenesis and growth. Most meningiomas are located in the anterior or middle skull base, where a higher prevalence of progesterone receptors has been observed. This evidence further underlines the relationship between hormonal factors and this type of intracranial tumor. Moreover, rapid and spontaneous tumor regression has been reported after cessation of treatment with exogenous hormones or when serum progestogen levels decrease due to physiological factors. This study aimed to investigate the presence of a safety signal for meningioma among users of estro-progestin and progestin-only therapies using pharmacovigilance data. Data from the EudraVigilance database were analyzed using both descriptive and statistical approaches. Three complementary disproportionality methods were applied to strengthen signal detection: Reporting Odds Ratio (ROR), Information Component (IC), and Empirical Bayes Geometric Mean (EBGM). The study period covered the last ten years, from January 1, 2016, to December 31, 2025. The drugs analyzed included: drospirenone-ethinylestradiol combination, dienogest-ethinylestradiol combination, drospirenone-only, desogestrel and levonorgestrel. We included all reports in which these drugs were recorded as suspected, excluding those in which they were reported only as concomitant drugs. A total of 21,091 reports, corresponding to 70,476 drug-ADR pairs, were identified. As expected, most reports concerned female patients, consistent with both the indication of these therapies and the known higher prevalence of meningioma in women. Disproportionality signals were identified for drospirenone and desogestrel-only formulations, suggesting a potential association with meningioma: A disproportionality signal was identified for desogestrel-only pills (110 reports; ROR 11.11, 95% CI 8.79-14.06; IC025 2.64; EB05 5.79). A novel exploratory signal also emerged for drospirenone-only pills (8 reports; ROR 2.41, 95% CI 1.19-4.89; IC025 0.54; EB05 1.17). No disproportionality signal was detected for the two combined formulations or levonorgestrel; absence of a signal should not be interpreted as absence of risk or evidence of comparative safety. In addition to meningioma, other serious adverse drug reactions - including known cardiovascular events and previously unreported reactions - were identified, warranting further investigation. These findings highlight the importance of ongoing pharmacovigilance activities and careful benefit-risk evaluation of hormonal therapies, particularly given their widespread and long-term use and the potential for rare but serious outcomes such as meningioma. This analysis identified new but exploratory safety signals that warrant confirmation in studies with valid exposure denominators, longitudinal treatment histories, latency assessment, and control of confounding. The findings should not be used alone to infer causality or guide comparative clinical decisions.

PMID 42925942
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PubMedFrontiers in medicine2026-10-23

Case Report: Distal ureteral obstruction decades after presumed intrauterine device removal in a woman with uterus didelphys.

Xiao Chengsheng C, Li Cheng C

An ectopic intrauterine device (IUD) can rarely cause ureteral obstruction and hydroureteronephrosis. Diagnosis may be delayed when a prior removal procedure is believed to have been complete. A 48-year-old woman presented with a 1-year history of right flank pain and urinary frequency after repeated treatment for presumed urinary tract infection and possible genitourinary tuberculosis without sustained improvement. More than 20 years earlier, an IUD had been inserted before uterus didelphys was recognized. Two to three years later, an unintended pregnancy led to recognition of the duplicated uterine anatomy, induced abortion, and an IUD removal procedure. The original records were unavailable, so device location and intact retrieval at that time could not be verified. Multimodality imaging at the index admission showed severe right hydroureteronephrosis, focal distal ureteral narrowing, and an ectopic metallic IUD outside both uterine cavities; cystoscopy was unremarkable. Open ureteral exploration and reconstruction identified an intact IUD with an attached calculus externally compressing an approximately 1-cm fixed distal ureteral stricture without entering the ureteral lumen. The narrowing persisted after device removal, requiring segmental ureteral resection and anastomosis over a double-J stent. Histopathology of the resected ureter showed chronic inflammatory changes without tuberculous changes. The stent was removed 2 months postoperatively. At 6 months after surgery, computed tomography showed marked decompression of the right collecting system and no residual pelvic metallic device; serum creatinine remained normal. A history of IUD removal should not be treated as proof of device absence when intact retrieval is undocumented. In otherwise unexplained unilateral ureteral obstruction, a remote IUD history should prompt review of prior device localization and targeted pelvic imaging, particularly when historical records are unavailable or duplicated uterine anatomy complicates localization. A fixed stricture may require reconstruction even after the ectopic device is removed.

PMID 42908971
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PubMedThe Journal of adolescent health : official publication of the Society for Adolescent Medicine2026-10-23

Comparative Efficacy of Medical Therapies for Heavy Menstrual Bleeding in Adolescents and Young Adults With Bleeding Disorders.

Huang He H, Isaacson Erin E, Weyand Angela C AC, McCracken Kate K et al.

Adolescent and young adult (AYA) females with bleeding disorders (BDs) frequently experience heavy menstrual bleeding (HMB), posing substantial clinical challenges. Data comparing the efficacy of specific hormonal treatment options in this population remain limited. We conducted a retrospective review of AYA females (≤21 years) with BD and HMB referred to a multidisciplinary Pediatric and Adolescent Gynecology-Pediatric Hematology joint clinic between November 2016 and December 2023. Treatment efficacy was defined as achieving a patient-reported significant reduction in or cessation of menstrual bleeding. The primary objective was to compare the efficacy of different hormonal and hemostatic therapies. Among 121 AYA females with BD, von Willebrand disease was the most common diagnosis (67.0%). HMB developed within 1 year of menarche in 79.3% of cases, and 73.6% received their BD diagnosis only after HMB onset. Combined estrogen-progestin oral contraceptive pills (OCPs) were the most common initial therapy (62.8%), yet 58.7% required switching to alternative regimens. Oral progestins demonstrated the highest efficacy (89.8%), followed by levonorgestrel-releasing intrauterine system (81.5%) and OCPs (65.5%). Only 17.4% achieved complete amenorrhea, though most experienced clinically meaningful bleeding reduction. Treatment efficacy differed significantly across modalities (p < .001). Progestin-based therapies, particularly norethindrone and norethindrone acetate, offer superior bleeding control and should be considered first-line treatment in AYA with BD. Levonorgestrel-releasing intrauterine system and OCPs are also effective alternatives. Given the difficulty of achieving complete amenorrhea, clinical goals should prioritize meaningful bleeding reduction that supports quality of life. Early multidisciplinary referral is recommended to optimize individualized care.

PMID 42911153
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PubMedAnnales d'endocrinologie2026-10-23

Cardiovascular and thromboembolic risks of sex hormone therapy: from contraception to transgender care.

Bonnet Fabrice F, Vaduva Patricia P, Dosda Arnaud A

The risk of venous thromboembolism is increased with combined oral contraceptives, rises with the dose of ethinylestradiol, and is higher with desogestrel, gestodene, drospirenone or cyproterone acetate than with levonorgestrel; the determinant is not the generation of the pill but the residual androgen-receptor activity of the progestin, which modulates the hepatic effect of the estrogen. Age over 35 years, obesity, smoking and a family history of thrombosis amplify it. Pills based on a native estrogen have a more limited hepatic impact and rank below most ethinylestradiol combinations in contemporary cohorts, but their clinical safety is not demonstrated and no comparative outcome data exist for estetrol/drospirenone. Androgenicity is not a general marker of venous safety: injectable depot medroxyprogesterone acetate, given alone at supraphysiological doses, carries an increased risk. Myocardial infarction and stroke are also more frequent, but against a very low background - about 21 additional strokes and 10 additional infarctions per 100,000 person-years, four times fewer than the venous excess - and, unlike venous events, independent of progestin type. Menopause hormone therapy increases venous thromboembolic risk, especially in the first year; the route of administration is the main determinant, transdermal estradiol with micronized progesterone appearing safest. In cisgender men, testosterone deficiency carries increased cardiovascular risk, and randomized and real-world data support the safety of transdermal replacement, although more pulmonary embolism and atrial fibrillation have been observed. In trans women, observational data show an increased risk of stroke and venous thromboembolism, particularly with oral estradiol and cyproterone acetate, whereas recent large-scale data show no excess of major cardiovascular events with testosterone in trans men. The practical consequences are specific: no combined pill is acceptable after a venous thromboembolic event, with a thrombogenic mutation or with migraine with aura, native-estrogen pills included; transdermal estradiol should be preferred for menopause and feminising hormone therapy; and haematocrit should guide the dose and route of testosterone.

PMID 42918571
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PubMedLancet (London, England)2026-10-22

Endometrial ablation plus levonorgestrel-releasing intrauterine system versus endometrial ablation alone in women with heavy menstrual bleeding in The Netherlands (MIRA2): a multicentre, open-label, randomised, controlled, superiority trial.

Oderkerk Tamara J TJ, Leemans Jaklien C JC, Beelen Pleun P, Herman Malou C MC et al.

Endometrial ablation is an established and effective treatment for women with heavy menstrual bleeding, but many patients require further treatment, with approximately 10% ultimately undergoing a hysterectomy within 2 years. The insertion of a levonorgestrel-releasing intrauterine system (LNG-IUS) immediately after endometrial ablation might inactivate residual untreated endometrium or prevent its regeneration, thereby preventing recurrent symptoms necessitating a hysterectomy. The aim of the study was to assess whether LNG-IUS insertion immediately after endometrial ablation in women with heavy menstrual bleeding reduced the need for subsequent hysterectomy within 2 years compared with endometrial ablation alone. This multicentre, open-label, randomised, controlled, superiority trial was conducted in 34 hospitals in the Netherlands. Women younger than 60 years with heavy menstrual bleeding who were eligible for endometrial ablation were included and randomly assigned (1:1) to combined treatment comprising endometrial ablation plus LNG-IUS or to standard care comprising endometrial ablation alone (stratified by dysmenorrhoea and age). Masking was not applied. Endometrial ablation was done using electrical radiofrequency ablation or by transcervical resection of the endometrium. In participants allocated to combined treatment, intrauterine insertion of an LNG-IUS containing a total of 52 mg of levonorgestrel (releasing 20 μg per day in the first year) was done immediately after the ablative procedure. The primary outcome was the incidence of hysterectomy within 2 years, analysed on a modified intention-to-treat basis in all participants with available data. Serious adverse events were systematically assessed at 6 weeks, 12 months, and 24 months after the intervention. This study was registered on the International Clinical Trials Registry Platform (NL-OMON54839) and is complete. Between Nov 19, 2019, and April 5, 2023, 715 participants were randomly assigned to combined treatment (n=359) or endometrial ablation alone (n=356). The median age of all participants was 45 years (IQR 40-48). 42 (6%) participants had missing data for the primary outcome at 2 years of follow-up. A hysterectomy was done in 15 (4%) of 342 participants in the combined treatment group versus 34 (10%) of 331 participants in the endometrial ablation group, corresponding to a relative risk (RR) of 0·43 (95% CI 0·24 to 0·77; p=0·0050), with a risk difference of -0·06 (95% CI -0·10 to -0·02; p=0·0040). Serious adverse events were reported in 27 (8%) of 346 participants in the combined treatment group and 26 (8%) of 327 participants in the endometrial ablation alone group (RR 0·98, 95% CI 0·59-1·65; p=0·94), and there were no treatment-related deaths. The combination of endometrial ablation and LNG-IUS significantly reduced the incidence of hysterectomy compared with endometrial ablation alone. The combined treatment appears to be a safe adjunctive strategy for heavy menstrual bleeding that does not increase the risk of complications. The Netherlands Organization for Health Research and Development.

PMID 42906565
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