TAK-385; Orgovyx; Relumina


For these patients who have few effective treatment options, there is great opportunity for novel drugs to have a big impact on outcomes and quality of life. With Relugolix, patients have an effective, oral choice, although with long-term hypoestrogeneic side effects that will need to be taken into consideration and potentially managed.

About relugolix

  1. Developed by Takeda Pharmaceutical Co Ltd and licensees Myovant Sciences Ltd, Pfizer Inc, ASKA Pharmaceutical Co Ltd and Gedeon Richter
  2. GnRH receptor antagonist

Relugolix for prostate cancer

  1. Approved for treatment of prostate cancer in the U.S. (December 2020) 
  2. Multicountry Phase 3 (HERO) trial ongoing in Australia, Brazil, Canada, Europe, Japan, Mainland China, New Zealand, South Korea and Taiwan

Relugolix for endometriosis

  1. Phase 3 trials ongoing in Australia, Canada, Japan, New Zealand, South Africa, South America and the United States

Relugolix for uterine fibroids

  1. Approved for treatment of uterine fibroids in Japan (February 2019)
  2. Undergoing MAA/NDA review by the EMA and U.S. FDA
  3. Phase 3 trials ongoing in Brazil, Chile and South Africa
expected sales in 2025

About the prostate cancer market

  1. Mainstay frontline treatment: androgen deprivation therapy, including orchidectomy, GnRH agonists and GnRH antagonists (administered alone or in combination with chemotherapy, radiotherapy or androgen antagonists)
  2. Primary competitors: Lupron depot (GnRH agonist), Firmagon (GnRH antagonist)
  3. Other drug classes used for treatment: chemotherapy, immunotherapy, bone metastases-targeted agents and PARP inhibitors
  4. Dynamic late-phase development pipeline that spans a wide range of drug classes, including novel classes, with significant potential for drug developers to target large number of drug-treatable cases of hormone-sensitive and castration-resistant prostate cancer (CRPC)
CAGR of diagnosed incident cases from 2019 to 2029, driving an increase in drug-treatable cases
CAGR: compound annual growth rate

Unmet patient needs

Patients with prostate cancer would benefit from therapies with greater effectiveness, targeting predictive biomarkers with new MOAs and that prevent or delay progression to CRPC.

most frequent malignancy in men worldwide

“Relugolix could be a huge game changer. …with Firmagon, there was a retrospective paper that showed less cardiovascular toxicity. Giving an agonist increases risks of heart attacks and cardiac death, but Firmagon will reduce this. To have an oral antagonist sounds amazing. I don’t think you could use relugolix for everybody…it is going to be more expensive than current therapies…a lot of men like having a three- or six-monthly injection over a daily tablet, but for those who have had a cardiovascular event or high-risk cardiac, I think you could probably…work out that you are actually saving money.”

Medical oncologist,
United Kingdom

About the endometriosis market

  1. Elagolix (Orilissa), an oral GnRH antagonist, first and only drug to be approved by the U.S. FDA (August 2018) to treat endometriosis-related pain
  2. Surgical options: excision or ablation, hysterectomy with concurrent oophorectomy
  3. First-line therapies for endometriosis-related pain: hormonal contraceptives and NSAIDs
  4. Second-line therapies for endometriosis-related pain: GnRH agonists (e.g., Lupron)
  5. Large drug-treated population as a sizable target for developers of novel therapies
of women with a confirmed endometriosis diagnosis are drug-treated

Unmet patient needs

There are few safe, long-term medical treatments, particularly non-hormonal or non-invasive options, for the management of endometriosis-related pain.

Many treatments have undesirable menopause-like side effects (hot flashes, headache, nausea). Due to an increasing proportion of women delaying childbearing until later in life, there is also demand for uterus-sparing treatments.

women aged 15-54 years worldwide have confirmed or suspected endometriosis

“Using birth control pills continuously can help the majority of the endometriosis-related pain. GnRH antagonists are likely to be used in the second line following birth control pills, and they have the potential for long-term use.”

United States

About the uterine fibroid market

  1. Elagolix (Oriahnn): first and only GnRH antagonist approved by the U.S. FDA (June 2020) to treat uterine fibroids
  2. Cornerstones of medical management for uterine fibroids: hormonal contraceptives, GnRH agonists, tranexamic acid, NSAIDs, leuprolide and ulipristal (Europe only)
  3. Surgical options: hysterectomy, myomectomy and minimally invasive procedures such as uterine artery embolization, myolysis and endometrial ablation 
Hysterectomy is currently the only definitive cure for uterine fibroids, but it also results in permanent loss of childbearing capability. 

Unmet patient needs

There are few safe, long-term medical treatments for uterine fibroid management, and rebound fibroid growth can occur once treatment ends.

Patients are reliant on therapies that are safe but less effective, are effective but with a suboptimal safety profile, or have menopause-like side effects (hot flashes, headache, nausea).

Due to an increasing proportion of women delaying childbearing until later in life, there is also demand for uterus-sparing treatments.

women aged 20-54 years worldwide have uterine fibroids

“I guess the only real benefit for GnRH antagonists is the fact that you can give them orally, as compared with the agonist where you have to usually use an injection. So, I think that’s the real benefit of the antagonists.”

United Kingdom

Why is it a drug to watch?

Its potential use for three indications increases its chances of success.

The oral formulation (daily administration) provides advantages over the injectable (administered every 3 months) GnRH agonist competitors, including convenience and better management of side effects.

Demonstrated to be efficacious and comparatively safe, relugolix provides another option for medical management and might prevent or delay the need for surgical treatment.

Insights from the analyst

What you need to know

For women with few effective medical management options for uterine fibroids and endometriosis, relugolix is promising for its efficacy and ease of use. However, long-term use of GnRH antagonists is hampered by hypoestrogenic side effects, including bone loss.

As the second-to-market GnRH antagonist for both endometriosis and uterine fibroids in the U.S., it will compete with AbbVie’s Orilissa/Oriahnn, which had combined sales of $125M in 2020.

Although it will be first to market in the E.U., it is a smaller commercial opportunity.

Its uptake for prostate cancer will likely be modest, despite its entry as the first and only GnRH antagonist approved for prostate cancer, owing to fierce competition from the well-established GnRH agonists and Firmagon (injectable GnRH antagonist), and sales will be further constrained by the expected entry of generic alternatives.

Numerous questions remain about the launch prospects for agents in this class, but signals of therapeutic potential from completed studies indicate clinical success in early Alzheimer’s disease remains possible with optimized treatment dosing and duration.

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