Relugolix: An Up-and-Coming Treatment for Endometriosis Symptoms?

a pill

You’ve more than likely heard of Elagolix, but have you heard of Relugolix? It’s a GnRH antagonist. And, yes, it’s the same classification of drug as Abbvie’s Elagolix (aka Orlissa). It’s being groomed to treat fibroids, prostate cancer, and (yep, you guessed it) Endometriosis pain.

Although not yet approved here in the United States, Japan approved Relugolix in January 2019 to treat uterine fibroids under the name Relumina. According to an Amsterdam company, TheSocialMedNework, Relumina is available for $1,400 for a box of 100 tablets (the standard dosage is one 40-mg tablet per day). I’m curious how that price rate would change in the United States if it were ever approved. It is expected that the FDA will receive an application for approval to treat uterine fibroids later this year.

And there’s an interesting race between Myovant Sciences and Abbvie. Elagolix (Orilissa) was approved last year to treat Endometriosis pain, but Abbvie will be seeking FDA approval for it to treat uterine fibroids as well. Myovant will be seeking FDA approval for Relagolix to treat uterine fibroids…and eventually Endometriosis pain. The race is on!

Common side effects include (I consider this list incomplete and will continue to search for information):

  • hot flashes
  • irregular uterine bleeding
  • heavy menstrual bleeding
  • headache
  • excessive sweating
  • genital bleeding
  • depression
  • liver function disorder

In 2016, it was reported (in the US Exchange & Securities Registration Statement) that out of 1,300 trial subjects, there were a total of 36 serious adverse events. Of those 36: “one event of abnormal liver function tests, one of cerebral infarction, and one of embolic stroke.” The investigator noted those three events may have been “possibly related to Relugolix.” Dr. Google tells me that cerebral infarction and embolic stroke have to do with a blockage of the blood supply to the brain.

Myovant Sciences is working on developing Relugolix in combination with estradiol and progestins to ease side effects and prevent bone loss. In the US Exchange & Securities Registration Statement by Myovant on July 8, 2016, they identify Relugolix as their “lead product candidate” and outline their prospective trial timetable. Myovant appears to be a small fish in the pharmaceutical sea with not a lot of products under their belt.

Clinical trials are ongoing around the world for its effectiveness against fibroids, endometriosis symptoms, and prostate cancer. The study for endometriosis is called Spirit. More information can be found on MySpiritStudy .

Following is a timeline of clinical trials of Relugolix pertaining to Endometriosis:

October 2011: Efficacy and Safety of TAK-385 (Relugolix) in the Treatment of Endometriosis. This study concluded in August of 2013, with 487 participants and tested the drug for 12 weeks or more in 10, 20, and 40mg doses, as well as had a placebo and Lupron Depot injections as comparison. It completed in August of 2013.

March 2012: A Long-term extension study of TAK-385 (Relugolix) in the Treatment of Endometriosis. This study had 397 participants and tested the drug for 12 weeks or more in 10, 20, and 40mg doses, as well as had a placebo and Lupron Depot injections as comparison. It completed in December 2013.

November 2017 and December 2017: Spirit 1 and Spirit 2: Efficacy and Safety Study of Relugolix in Women with Endometriosis-Associated Pain. Still actively recruiting, these study hope to conclude by June 2020. They seek to have at least 1,200 participants testing Relugolix for 24 weeks; some with the drug and added estradiol/progestins; and others with Relugolix and placebo.

May 2018: Spirit Extension: Efficacy and Safety Extension Study of Relugolix in Women with Endometriosis-Associated Pain. This study is ongoing (by invitation only) and expected to be complete in mid-2022. They are hoping to have at least 800 participants to evaluate 40mg Relugolix in combination with estradiol and norethindrone acetate for up to 28 weeks.

May 2019: Clinical Study to Evaluate Efficacy of TAK-385 40mg Compared with Leuprorelin in Patients with Endometriosis. Presently recruiting, this study wants to have 320 participants and compare Relugolix to Lupron Depot for 24 weeks. They hope to have this study completed by early 2021.

Studies have shown that women have reported less pelvic pain when taking 40mg of Relugolix compared to the placebo.

If you’ve participated in these studies, please respect the non-disclosure agreements I’m sure you had to sign and refrain from commenting on your experience. Although I am mightily curious! But, I absolutely respect the NDAs.

I look forward to more information becoming available on the clinical trial outcomes, and a more thorough identification of the adverse side effects. Will I use it? More than likely not just because of the nature of the beast that it is. Lupron was similar…and was not a pleasant journey for me. But will I dissuade you from trying it IF it ever hits our shelves. Never. I’ll simply ask you to do your research first.

Resources:

BiopharmadiveMyovant Reports a Phase 3 Success, but Wall Street Isn’t Cheered

Biopharmadive Myovant Set to Battle Abbvie After Second Phase 3 Success for Key Drug

Clinical Trials

Drugs (Abstract; April 2019) – Relugolix: First Global Approval

Endometriosis News Relugolix

Myovant SciencesRelugolix

Roivant Sciences (Article; May 2017) Myovant Sciences Announces Presentation of Positive Phase 2 Date for Relugolix in Women with Endometriosis-Associated Pain at the World Congress on Endometriosis

TheSocialMedNetworkRelumina

US Securities and Exchange Commission – Myovant Sciences, Ltd’s Registration Statement

Wikipedia Relugolix

~ Again, I am a layman. I do not hold any college degrees, nor mastery of knowledge. Please take what I say with a grain of salt. If curious, do your own research. Validate my writings. Or challenge them. And ALWAYS feel free to consult with your physician. Always. Yours ~ Lisa

Lupron Depot: Q&A

Q&A

As many of you know, I was on Lupron Depot for six months for my Endometriosis.  I wrote about my personal experiences here and also how my life had changed after my last injection (you can read that, and other’s experiences, here).

Recently, a friend of mine learned he will be starting Lupron Depot to treat his prostate cancer.  My husband was surprised this morning when I told him.  He didn’t realize the drug’s original purpose was to treat cancer…in men!  And it’s because of the connection with cancer that many people think Lupron Depot is chemotherapy.  It isn’t.

So, today’s blog entry is here to accomplish a few things:

  1. Discuss the origins and history of Lupron Depot;
  2. How it morphed from a cancer treatment to a treatment for hormonal issues (such as Endometriosis, fibroids, and central precocious puberty); and,
  3. Clarify why I think Lupron Depot is not considered chemotherapy.

I am in no way encouraging or discouraging the use of Lupron Depot in your treatment regimen.  This will not be a commentary piece about the pros & cons of the drug.  The decision is yours.  Research the drug, the side effects, and have lengthy discussions with your physician.

Let the research begin!!

What is Lupron Depot?  In a nutshell, it’s a drug delivered by injection that shuts off your hormones.  In men, testosterone; in women, estrogen.  It’s not an easy treatment to endure, that’s for sure…but every person is different in how their body reacts to the drug.

When was Lupron Depot created?

In 1977, two companies, Takeda (Japan) and Abbott Laboratories (USA), came together and formed TAP Pharmaceuticals, Inc.

In 1985, Lupron Depot was approved for the American market to treat prostate cancer.  Over the years, label improvements, dosage changes, and  better syringes were approved by the FDA.

In 2008, Takeda and Abbott ended their joint venture of TAP Pharmaceuticals.  Abbott Laboratories retained “the Lupron franchise.”

In 2013, AbbVie emerged from Abbott Laboratories and took over the manufacture and distribution of Lupron Depot.

When was it approved for prostate cancer treatment?

In 1985, Lupron Depot was approved to treat prostate cancer.

If it’s not chemotherapy, what is it?

I’ve talked to nurses and doctors about this question multiple times.  I’ve done research.  And I am strongly opinionated on the subject.

It’s a hormone therapy drug.  It works with the pituitary gland and shuts down the body’s ability to produce testosterone or estrogen.  That suppression, in theory, gives the body a fighting chance at beating the cancer because those cells are no longer being fed the hormone it desires so badly to grow.  Lupron Depot does nothing to physically attack cancer.  It simply alters the body’s ability to create hormones that may feed cancer cells.  This starvation effect can either slow or shrink the cancerous growths.

It is not chemotherapy.  I repeat: it is not chemotherapy.

Chemotherapy medications attack the cancer cells directly.  Lupron Depot is a supportive medication that may starve the cancer cells.  It’s like comparing apples and oranges.

When was it approved for Endometriosis treatment?

The best I can find, Lupron Depot was approved by the FDA in 1990 for treating Endometriosis.

When was it approved for Central Precocious Puberty?

In 1993, Lupron Depot-PED was approved by the FDA to treat a childhood hormonal imbalance called Central Precocious Puberty.  What’s CPP?  It’s when children who are younger than 8 or 9 years old (depending on their sex) show signs of puberty and sexual maturity.  Lupron Depot suppresses the hormones, thus suppressing the pace of puberty.

[I know I said I would keep the commentary to myself, but I have to voice this one: I could not even imagine a child going through the side effects I went through…breaks my heart.]

There!  I’ve accomplished what I set out to do today.  *whew* If you’re reading this and I got my dates wrong, please feel free to correct me.  If you’d like to express how Lupron Depot has affected YOUR life, please do so by clicking here.

Resources:

AbbVie.com

Chemocare.com

Chemotherapy.com

Crunchbase.com

CVS.com

Endofacts.com

FDA (1993)

FDA (1995)

FDA (1998)

FDA (2001)

Genetics Home Research

Gregthatcher.com

Lupron.com

LupronPED.com

LupronProstateCancer.com

LupronProstateCancer.com – timeline video

LupronVictimsHub.com

Takeda.com

~ Again, I am a layman.  I do not hold any college degrees, nor mastery of knowledge.  Please take what I say with a grain of salt.  If curious, do your own research 😉 Validate my writings.  Or challenge them.  And ALWAYS feel free to consult with your physician. Always.  Yours ~ Lisa

 

Share Your Story : Terry

lupron

Today’s story is a bit different.  Meet, Terry, a 72-year-old man from California.  Terry was diagnosed with prostate cancer and was prescribed Lupron Depot as part of his treatment.  He would like to share his experience with us today, as well as pose a question to all of you:

*

I had prostate cancer and opted for the radiation (43 days) and Lupron Injections for two years – every six months. I was able to withstand the first two injections but the side effects were so bad, I told the doctor to discontinue.

I was due for my third injection on June 15th, 2016 – its now August 6th and I still have side effects. At the height of my pain, there were hot flashes, joint pain in hips, knees, feet, chills, fatigue, burning urine, loose bowels, and would get up 10 times at night. Some of the side effects have decreased, however, the fatigue is extreme. Still having to go to the bathroom all through the night and loose bowels.

The doctors never mentioned any of the less common side effects. Hopefully, it gets better?

*

If YOU would like to give Terry some encouragement and discuss your side effects and how long they took to dissipate (assuming they have), please email him here.  He would love some hope and encouragement.  And I know so many of you who offer hope and encouragement.

And if you would like to share your story, click here.