First enrollment! The novel GnRH antagonist, Linzagolix, will break the current situation of patients with uterine fibroids who lack drugs that can be taken orally for a long time and have flexible dosage regimens Press Release

On December 16, 2022, Shanghai Baozheng Pharmaceutical Technology Co.
, Ltd.
(hereinafter referred to as "Baozheng Pharmaceutical") announced that its bid for BG2109 (Linzagolix) for the treatment of excessive menstrual bleeding associated with uterine fibroids in premenopausal women (drug clinical trial registration platform: CTR20221747) welcomed the first subject enrollment
.

Linzagolix is a novel, oral, non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist.

THE DRUG WAS ORIGINALLY DEVELOPED BY KISSEI PHARMACEUTICAL CO.
, LTD.
OF JAPAN, AND BAOZHENG PHARMACEUTICAL OBTAINED THE EXCLUSIVE DEVELOPMENT RIGHT
OF THE DRUG IN GREATER CHINA.
Linzagolix will fill the gap in the clinical treatment of uterine fibroids in China: providing safe and efficient non-surgical long-term management solutions
for clinical practice.

Linzagolix is taken orally once daily to treat estrogen-dependent diseases
by inhibiting the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) by inhibiting the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) and reducing estrogen levels.
In June 2022, Linzagolix tablets (trade name Yselty^®) were approved in the European Union and the United Kingdom for the treatment of moderate to severe symptoms of uterine fibroids in women of childbearing age, including 100mg and 200mg, which can be used alone or in combination with reverse estrogen and progesterone therapy (ABT), except for 200mg alone is approved for short-term treatment (< 6 months) to reduce the volume of uterine and fibroids <b12>[1，2]
。 As a result, Linzagolix becomes the world's first approved and only GnRH antagonist
that offers flexible dosage options.

At present, similar drugs that have been marketed overseas to treat severe symptoms of uterine fibroids include Elagolix (trade name ORIAHNN^®) and Relugolix (trade name MYFEMBREE^®), both fixed dosage forms containing hormone ABT, and the maximum course of treatment is not more than 24 months ^[3,4].

。 In contrast, Linzagolix is also suitable for patients who do not receive or are not candidates for hormonal ABT therapy, has a broader target population, and offers a variety of options for short-term use and/or long-term maintenance therapy to better meet the individual needs
of patients.

The Lancet, the world's top medical journal, recently published the results of two core global phase III clinical trials (PRIMROSE 1 and 2 studies) of Linzagolix for the treatment of uterine fibroids ^[5].

。 The proportion of patients who met the primary endpoint of a decrease in menstrual bleeding (i.
e.
, ≤80 mL and a ≥50% reduction from baseline) at 24 weeks in all doses of once-daily oral Linzagolix was significantly higher than in the placebo group (P≤0.
003), with the highest achievement rates of 75.
5% and 93.
9%,
respectively, in the 200 mg plus ABT group 。 The Linzagolix 200 mg group also significantly reduced uterine and fibroid volume, with mean uterine volume reduced by 31% and 43% and average fibroid volume by 45% and 49%
in participants in both studies at 24 weeks of treatment.
Linzagolix had a good overall safety and tolerability and no serious adverse events
were noted.

Professor Xu Congjian, principal investigator of Linzagolix phase III clinical trial of uterine fibroids in China and president of Fudan University Obstetrics and Gynecology Hospital, pointed out:

Symptomatic uterine fibroids seriously affect the reproductive health of women of childbearing age, reduce work efficiency and quality of life, and drug treatment should become an important option
for their clinical treatment.
In the clinical practice of obstetrics and gynecology, patients should be the centered, and the individualized, safe, efficient, economical and convenient drug treatment regimen for symptomatic uterine fibroids should be continuously explored
.
Baozheng Medicine introduced Linzagolix, an overseas original GnRH antagonist, which is reported in foreign literature not only in the treatment of excessive menstrual bleeding associated with uterine fibroids, but also in reducing pain, reducing the volume of uterine and fibroids, improving anemia, and improving quality of life ^[5].

As the only oral GnRH antagonist in the world that can provide flexible dosage regimens, doctors can choose individualized regimens according to different patients' different conditions, which is expected to fill clinical gaps
.
It is expected that the phase III trial in China will be carried out smoothly and approved for marketing as soon as possible, benefiting the majority of uterine fibroid patients
.

Ji Baohua, founder of Baozheng Pharmaceutical, said:

Baozheng Pharma focuses on women's health in China, deeply cultivates the field of gynecology and reproductive health with huge unmet clinical needs, deeply understands women's needs and clinical challenges, and is committed to providing comprehensive solutions
to women's health problems.
At present, through the promotion of independent research and development and introduction of two-wheel drive, it has built a clinical and commercial platform
for the research and development of drugs, health products and medical devices.
Uterine fibroids and endometriosis account for two of the top three disease burdens in women of childbearing age in China ^[6].

Therefore, the first introduction of Linzagolix core products will provide better treatment options for female diseases such as uterine fibroids, endometriosis, and assisted reproduction (treatment
of infertility).
Baozheng Pharmaceutical will continue to solve clinical pain points, actively respond to and implement the State Council's "Outline for the Development of Chinese Women (2021-2030)" and "Outline for the Development of Chinese Children (2021-2030)", and enhance the sense of gain, happiness and security of the majority of women
.

About uterine fibroids

Uterine fibroids are the most common benign tumors in women, with an estimated prevalence of up to 25 percent in women of childbearing age ^[7], and estrogen levels are important factors
in regulating fibroid growth in addition to genetic factors.
Uterine fibroids can cause abnormal uterine bleeding, severe menstrual bleeding, secondary anemia, and in severe cases life-threatening, with abdominal and pelvic compression symptoms, abdominal pain, and may lead to infertility ^[7,8].

At present, the main treatment method in China is surgery, but the recurrence rate after surgery is close to 50%, and about 1/3 of patients need to be reoperated ^[7], and total hysterectomy will make patients lose their fertility
.
Commonly used clinical drugs are mainly proprietary Chinese medicines, as well as hormonal contraceptives, nonsteroidal anti-inflammatory drugs, tranexamic acid and other symptomatic drugs
.
Subcutaneous injection of GnRH agonist has a "ignition" effect, that is, the original symptoms are aggravated in the early stage of treatment, and the short-term use is limited to 3~6 months due to the significant risk of bone loss, etc.
, and the uterine fibroids tend to "rebound" to the pre-treatment size after stopping the drug ^[7], so it is mostly used as an adjunct to reduce the volume of fibroids before surgery
.

Source