In 2015, ObsEva in-licensed Linzagolix for the treatment of endometriosis from Kissei Pharmaceutical Co.
Linzagolix is a novel, oral gonadotropin-releasing hormone (GnRH) receptor antagonist that potentially provides effective management of heavy menstrual bleeding (HMB) associated with uterine fibroids (UF) while mitigating bone mineral density loss and other adverse effects typically associated with currently approved treatments. Unlike many currently marketed GnRH agonists, Linzagolix has the potential to be administered orally once a day, with symptoms relieved within days, while potentially mitigating the initial worsening of symptoms often associated with GnRH agonist treatments. In contrast to other GnRH receptor antagonists in development, Linzagolix has innovative properties that have the potential to allow for personalized dosing that can be tailored to a patient’s individual response. This means that Linzagolix has the potential to lower estradiol levels while maintaining such levels within an optimal range to mitigate patient bone mineral density loss. Linzagolix has the potential to allow patients to receive the relief needed to live normal lives again and enhance their quality of life with fewer side effects and complications requiring doctor’s visits or surgery.
In a Phase 2a clinical trial, which included a subgroup of patients with both endometriosis and UF, Linzagolix provided significant, dose-dependent decreases in serum LH and estradiol levels in UF patients. This resulted in the reduction of bleeding days within the first month of treatment (>90 percent of patients) and anemia correction within three months (>90 percent of patients) of treatment.
In April 2017, ObsEva commenced the PRIMROSE 1 and 2 clinical trials of Linzagolix in women with heavy menstrual bleeding (HMB) associated with uterine fibroids (UF). These Phase 3 trials are presently screening and enrolling patients.
View Linzagolix publications here.
View Clinical Trials:
In 2015, ObsEva in-licensed Linzagolix from Kissei Pharmaceutical Co., which had completed several Phase 2a clinical trials in Japan.
Linzagolix is a novel, oral gonadotropin-releasing hormone (GnRH) receptor antagonist that potentially provides effective management of endometriosis-associated pain while mitigating bone mineral density loss and other adverse effects typically associated with currently approved treatments. Unlike many currently marketed GnRH agonists, Linzagolix has the potential to be administered orally once a day, with symptoms relieved within days, while potentially mitigating the initial worsening of symptoms often associated with GnRH agonist treatments. In contrast to other GnRH receptor antagonists in development, Linzagolix has innovative properties that have the potential to allow for personalized dosing that can be tailored to a patient’s individual response. This means that Linzagolix has the potential to lower estradiol levels while maintaining such levels within an optimal range to mitigate patient bone mineral density loss. Linzagolix has the potential to allow patients to receive the relief needed to live normal lives again and enhance their quality of life with fewer side effects and complications requiring doctor’s visits or surgery.
In a Phase 2a clinical trial, Linzagolix provided significant, dose-dependent decreases in serum LH and estradiol levels in patients with endometriosis. These patients experienced a reduction of disease-associated pain and bleeding days, as well as improved quality of life (>85 percent). The use of Linzagolix also led to a significant dose-dependent reduction in the use of pain medication to manage endometriosis symptoms, as compared to patients in the placebo group.
EDELWEISS, a Phase 2b clinical trial of Linzagolix, as compared to placebo in endometriosis is underway in the US and Europe.
View Linzagolix publications here.
View Clinical Trial: