[1] OKADA H. One-and three-month release injectable microspheres of the LH-RH superagonistleuprorelin acetate[J]. Adv Drug Deliv Rev, 1997, 28(1):43-70.
[2] NCCN Clinical Practice Guidelines in Oncology. Breast Cancer, Version 2.2022[S/OL].[2022-03-10]. https://www.nccn.org/professionals/physician_gls/pdf/breast.pdf.
[3] NCCN Clinical Practice Guidelines in Oncology. Prostate Cancer, Version 3.2022[S/OL].[2021-03-10]. https://www.nccn.org/professionals/physician_gls/pdf/prostate.pdf.
[4] Chinese Society of Obstetrics and Gynecology of Chinese Medical Association, Chinese Obstetricians and Gynecologists Association Endometriosis Group. Guideline for the diagnosis and treatment of endometriosis(Third edition)[J]. Chin J Obstet Gynecol(中华妇产科杂志), 2021, 56(12):812-824.
[5] ZHOU Y F, LANG J H, BAI W P, et al. Chinese expert consensus on the diagnosis and treatment of uterine fibroids[J]. Chin J Obstet Gynecol(中华妇产科杂志), 2017, 52(12):793-800.
[6] Chinese Society of Pediatric Endocrinology and Metabolism. Chinese expert consensus on the diagnosis and treatment of central precocious puberty[J]. Chin J Pediatr(中华儿科杂志), 2015, 53(6):412-418.
[7] KATSUNO M, BANNO H, SUZUKI K, et al. Efficacy and safety of leuprorelin in patients with spinal and bulbar muscular atrophy(JASMITT study): a multicentre, randomised, double-blind, placebo-controlled trial[J]. Lancet Neurol, 2010, 9(9):875-884.
[8] LIU J, TU J S. Progress of the clinical application and the drug delivery system of leuprorelin acetate[J]. Pharm Clin Res(药学与临床研究), 2009, 17(4):309-311.
[9] WEI L M, SONG S K, SONG X. New developments in preparation methods of microspheres[J]. China Pharm(中国药师), 2011, 14(11):1682-1685.
[10] REN H X, ZHU J B, TANG Y. Advances of microsphere agents in application[J]. Prog Pharm Sci(药学进展), 2007, 31(2):59-63.
[11] CHAUDHARY K, PATEL M M, MEHTA P J. Long-acting injectables: current perspectives and future promise[J]. Crit Rev Ther Drug Carr Syst, 2019, 36(2):137-181.
[12] SUN Y, TANG S F, WANG W, et al. Quality review and analysis of leuprorelin acetate sustained release microspheres for injection[J]. Chin J Pharm Anal(药物分析杂志), 2020, 40(6):964-970.
[13] MEI X G, HUANG S H, BAI C Z. Worldwide development status of injectable microspheres for sustained release[J]. Chin J Drug Eval(中国药物评价), 2014, 31(1):27-28.
[14] QIU X M, ZHEN P, LI S K. Current advances in the drug-loading preparation of poly(lactic-co-glycolic acid) microspheres[J]. Chin J Tissue Eng Res(中国组织工程研究), 2018, 22(10):1599-1604.
[15] PARK K, SKIDMORE S, HADAR J, et al. Injectable, long-acting PLGA formulations: Analyzing PLGA and understanding microparticle formation[J]. J Controlled Release, 2019, 304:125-134.
[16] MAKADIA H K, SIEGEL S J. Poly Lactic-co-glycolic acid(PLGA) as biodegradable controlled drug delivery carrier[J]. Polymers(Basel), 2011, 3(3):1377-1397.
[17] HANSEN B, MATYTSINA I. Insulin administration: selecting the appropriate needle and individualizing the injection technique[J]. Expert Opin Drug Deliv, 2011, 8(10):1395-1406.
[18] HIRSCH L J, GIBNEY M A, ALBANESE J, et al. Comparative glycemic control, safety and patient ratings for a new 4 mm x 32G insulin pen needle in adults with diabetes[J]. Curr Med Res Opin, 2010, 26(6):1531-1541.
[19] SCHWARTZ S, HASSMAN D, SHELMET J, et al. A multicenter, open-label, randomized, two-period crossover trial comparing glycemic control, satisfaction, and preference achieved with a 31 gauge x 6 mm needle versus a 29 gauge x 12.7 mm needle in obese patients with diabetes mellitus[J]. Clin Ther, 2004, 26(10):1663-1678.
[20] TOSHIRO H, HIROAKI O, YUSUKE T, et al. Effects of counteranion of TRH and loading amount on control of TRH release from copoly(dl-lactic/glycolic acid) microspheres prepared by an in-water drying method[J]. Int J Pharm, 1991, 69(1):69-75.
[21] SIEGEL R A, LANGER R. Controlled release of polypeptides and other macromolecules[J]. Pharm Res, 1984, 1(1):2-10.
[22] OGAWA Y, YAMAMOTO M, OKADA H, et al. A new technique to efficiently entrap leuprolide acetate into microcapsules of polylactic acid or copoly(lactic/glycolic) acid[J]. Chem Pharm Bull(Tokyo), 1988, 36(3):1095-1103.
[23] Shanghai Livzon Pharmaceutical Co. Ltd. Method for preparing leuprolide acetate microspheres: China, 201310141233.9[P]. 2013-07-24.
[24] PENG Q, SONG N, MA W, et al. Advanced studies on influence factors on encapsulation efficiency and particle size of PLGA microspheres[J]. Prog Mod Biomed(现代生物医学进展), 2015, 15(29):5790-5793.
[25] LINA D, CHENG J P, CHI Q, et al. Biodegradable PLGA microspheres as a sustained release system for a new luteinizing hormone-releasing hormone(LHRH) antagonist[J]. Chem Pharm Bull(Tokyo), 2006, 54(9):1259-1265.
[26] Ch.P(2020) Vol Ⅳ(中国药典2020年版.四部)[S]. 2020:474-476.
[27] XIE L G, LIU Y L. Progress of controlling strategies for burst release of sustained-release injectable microspheres loaded with proteins[J]. Chin J Pharm(中国医药工业杂志), 2006, 37(9):639-643.
[28] ZHAO X Y, GAO J N, SU Y P, et al. Burst release and control of the delivery system of protein/peptide drug loaded poly(lactic-co-glycolic acid) microspheres[J]. J Clin Rehabil Tiss Eng Res(中国组织工程研究与临床康复), 2011, 15(38):7177-7180.
[29] O′HAGAN D T, JEFFERY H, DAVIS S S. The preparation and characterization of poly(lactide-co-glycolide) microparticles: Ⅲ. Microparticle/polymer degradation rates and the in vitro release of a model protein[J]. Int J Pharm, 1994, 103(1):37-45.
[30] PERITI P, MAZZEI T, MINI E. Clinical pharmacokinetics of depot leuprorelin[J]. Clin Pharmacokinet, 2002, 41(7):485-504.
[31] FREDENBERG S, WAHLGREN M, RESLOW M, et al.The mechanisms of drug release in poly(lactic-co-glycolic acid)-based drug delivery systems-a review[J]. Int J Pharm, 2011, 415(1-2):34-52.
[32] TUNN U W, BARGELLONI U, COSCIANI S, et al. Comparison of LH-RH analogue 1-month depot and 3-month depot by their hormone levels and pharmacokinetic profile in patients with advanced prostate cancer[J]. Urol Int, 1998, 60(Suppl 1):9-17.
[33] KUREBAYASHI J, TOYAMA T, SUMINO S, et al. Efficacy and safety of leuprorelin acetate 6-month depot, TAP-144-SR(6M), in combination with tamoxifen in postoperative, premenopausal patients with hormone receptor-positive breast cancer: a phase III, randomized, open-label, parallel-group comparative study[J]. Breast Cancer, 2017, 24(1):161-170.
[34] Chinese Urological Association, China Anti-Cancer Association-Genitourinary Cancer Committee, Chinese Urological Doctor Association. Chinese experts consensus on the testosterone therapy of prostate cancer(Version 2021)[J]. Chin J Urol(中华泌尿外科杂志), 2021, 42(4): 241-245.
[35] KIM H J, LEE J S, PARK E H, et al. Short term results from GHRH analogue use in pre-menopausal breast cancer in Korea[J]. Eur J Surg Oncol, 2009, 35(9): 936-941.
[36] AYDINER A, KILIC L, YILDIZ I, et al. Two different formulations with equivalent effect-comparison of serum estradiol suppression with monthly goserelin and trimonthly leuprolide in breast cancer patients[J]. Med Oncol, 2013, 30(1): 354. Doi:10.1007/S12032-012-0354-1.
[37] LEE Y J, WU Z Y, KIM H J, et al. Change in estradiol levels among premenopausal patients with breast cancer treated using leuprolide acetate 11.25 milligrams 3-month depot and tamoxifen[J]. J Breast Cancer, 2020, 23(5): 553-559.
[38] MA L X X, ZUO W J, MO M, et al. Comparison of the efficacy and safety of 3-month sustained releasing gonadotropin releasing hormone agonists and 1-month sustained releasing gonadotropin releasing hormone agonists in treating early breast cancer: a Bayesian network meta-analysis.[J]. Chin J Evid Based Med(中国循证医学杂志), 2022, 22(1): 37-45.
[39] FAN L, YEH Y C, DU F, et al. Cost comparison between leuprolide 3-month formulation and goserelin 1-month formulation as adjuvant endocrine therapy in post-mastectomy, premenopausal women with early-stage, estrogen receptor-positive breast cancer who are at moderate-to-high risk of recurrence in China[J]. China J Pharm Econ(中国药物经济学), 2020, 15(4): 5-10.
[40] CHEN Y F, YAN Y, JIANG H F, et al. Ovarian suppression efficacy of gonadotropin releasing hormone agonists for patients with premenopausal hormone receptor positive breast cancer: a real world study[J]. Mil Med Sci(军事医学), 2021, 45(5): 373-379.
[41] SONG G, GAO H, YUAN Z. Effect of leuprolide acetate on ovarian function after cyclophosphamide-doxorubicin-based chemotherapy in premenopausal patients with breast cancer: results from a phase II randomized trial[J]. Med Oncol, 2013, 30(3): 667. Doi:10.1007/S12032-013-0667-8.
[42] CHEN M L, LIN H Y, WU F, et al. Ovarian protective effect of leproteroline on breast cancer patients during chemotherapy[J]. Chin J Clin Pharmacol(中国临床药理学杂志), 2021, 37(19): 2581-2583.
[43] MARBERGER M, KAISARY A V, SHORE N D, et al. Effectiveness, pharmacokinetics, and safety of a new sustained-release leuprolide acetate 3.75-mg depot formulation for testosterone suppression in patients with prostate cancer: a Phase III, open-label, international multicenter study[J]. Clin Ther, 2010, 32(4): 744-757.
[44] SHORE N D, GUERRERO S, SANAHUJA R M, et al. A new sustained-release, 3-month leuprolide acetate formulation achieves and maintains castrate concentrations of testosterone in patients with prostate cancer[J]. Clin Ther, 2019, 41(3): 412-425.
[45] PIECZONKA C M, TWARDOWSKI P, RENZULLI J, 2ND, et al. Effectiveness of subcutaneously administered leuprolide acetate to achieve low nadir testosterone in prostate cancer patients[J]. Rev Urol, 2018, 20(2): 63-68.
[46] SHIM M, BANG W J, OH C Y, et al. Effectiveness of three different luteinizing hormone-releasing hormone agonists in the chemical castration of patients with prostate cancer: Goserelin versus triptorelin versus leuprolide[J]. Investig Clin Urol, 2019, 60(4): 244-250.
[47] LUO X, HOU L, ZHONG Y, et al.An open label, multicenter clinical trial that investigated the efficacy and safety of leuprorelin treatment of central precocious puberty in Chinese children[J]. Medicine(Baltimore), 2021, 100(51): e28158.
[48] CAREL J C, LAHLOU N, JARAMILLO O, et al. Treatment of central precocious puberty by subcutaneous injections of leuprorelin 3-month depot(11.25 mg)[J]. J Clin Endocrinol Metab, 2002, 87(9): 4111-4116.
[49] FULD K, CHI C, NEELY E K. A randomized trial of 1-and 3-month depot leuprolide doses in the treatment of central precocious puberty[J]. J Pediatr, 2011, 159(6): 982-987 e1.
[50] LEE P A, KLEIN K, MAURAS N, et al. 36-month treatment experience of two doses of leuprolide acetate 3-month depot for children with central precocious puberty[J]. J Clin Endocrinol Metab, 2014, 99(9): 3153-3159.
[51] QIN M, CAO W, ZHENG L, et al. Pharmacoeconomic evaluation of different gonadotropin releasing hormone analogs in the treatment of children with central precocious puberty[J]. China J Pharm Econ(中国药物经济学), 2021, 16(11): 10-14,24.
[52] ALKATOUT I, METTLER L, BETETA C, et al. Combined surgical and hormone therapy for endometriosis is the most effective treatment: prospective, randomized, controlled trial[J]. J Minim Invasive Gynecol, 2013, 20(4): 473-481.
[53] SOLIMAN A M, BONAFEDE M, FARR A M, et al. Analysis of subsequent surgery rates among endometriosis patients who underwent surgery with and without concomitant leuprolide acetate therapy[J]. Curr Med Res Opin, 2016, 32(6): 1073-1082.
[54] FULDEORE M J, MARX S E, CHWALISZ K, et al. Add-back therapy use and its impact on LA persistence in patients with endometriosis[J]. Curr Med Res Opin, 2010, 26(3): 729-736.
[55] JIANG S S, HU J H, SHEN Y. Clinical observation of laParoscoPic myomectomy combined with PreoPerative GnRH-a in treating leiomyoma with large uterus[J]. China J Endosc(中国内镜杂志), 2017, 23(5): 1-4.
[56] BIAN L H, WANG N, FAN W S, et al.Efficacy of GnRH-a in the prevention of recurrence of uterine myoma after laparoscopic myomectomy[J]. Acad J Chin PLA Med Sch(解放军医学院学报), 2017, 38(3): 199-201.
[57] HASHIZUME A, FISCHBECK K H, PENNUTO M, et al. Disease mechanism, biomarker and therapeutics for spinal and bulbar muscular atrophy(SBMA)[J]. J Neurol Neurosurg Psychiatry, 2020, 91(10): 1085-1091.
[58] LU M, FAN D S, SONG H S, et al. Leuprorelin in patients with spinal and bulbar muscular atrophy: an open study[J]. Chin J Neurol(中华神经科杂志), 2013, 46(8): 544-545.
[59] BANNO H, KATSUNO M, SUZUKI K, et al. Phase 2 trial of leuprorelin in patients with spinal and bulbar muscular atrophy[J]. Ann Neurol, 2009, 65(2): 140-150.
[60] HASHIZUME A, KATSUNO M, SUZUKI K, et al. Long-term treatment with leuprorelin for spinal and bulbar muscular atrophy: natural history-controlled study[J]. J Neurol Neurosurg Psychiatry, 2017, 88(12): 1026-1032.
[61] National Health Commission of the People′s Republic of China. Guideline for the diagnosis and treatment of rare diseases(Version 2019)[EB/OL].[2019-02-27]. http://www.nhc.gov.cn/yzygj/s7659/201902/61d06b4916c348e0810ce1fceb844333/files/e2113203d0bf45d181168d855426ca7c.pdf.