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

A beautiful breakdown of treatment options for Endometriosis

A pile of open books
Photo by Amanda George from Pexels

A new study about Endometriosis is out regarding the modern treatment of the disease.  This includes birth control, progestins/anti-progestins, GnRH agonists, aromatase inhibitors, danazol, NSAIDs, surgery, and alternative treatments. It identifies the pros and cons of each.

The study closes with this beautiful phrase:

“The pharmaceutical or surgical treatment require an individual approach and deliberated informed consent of the patient. Pharmacological treatment is only symptomatic, not cytoreductive, therefore, to remove endometriosis lesions, surgery should be performed.”

It’s uplifting to see a study bluntly state that medications only treat the symptoms, NOT the disease itself, and the Endo lesions need to be removed.  AND that each case of Endometriosis must be reviewed on an individual level.

Deliberated informed consent of the patient” means (to me) as having a fully-informed patient who is made well-aware of the pros and cons of each choice, the side effects, risks, and potential outcomes; as well as having performed their own research before agreeing to the treatment.

Even with excision, though, there’s always a possibly of recurrence or new growths. And not all physicians are skilled enough to recognize each lesion. Not to mention many surgeons still practice ablation (the burning away of the lesion, leaving rooted tissue to regrow).

Welcome to an EndoWarrior’s very frustrating pursuit for competent medical care.

I encourage you to read the study for yourself and share it.

Resources:

Journal of Education, Health, and Sport (Article, 2019) – Available Treatment Methods for Endometriosis

New Study: Elagolix vs. Lupron (Cost Effectiveness & Quality of Life)

Red apple and green apple
Comparing apples to…apples? Image by Freestocks.org

This will be a highly-charged opinion piece for me…so as you read what I am writing, please know that I am seething and upset and just needed to vent.

A study of Elagolix (aka Orilissa) hit my inbox recently and I just opened it today. It was run by Abbvie, of course. And it compares Elagolix to Lupron to see which is more cost-effective in possibly giving women with Endo a greater quality of life. So, it’s win-win for Abbvie since they make both of those drugs…

Elagolix was deemed the “winner” in that it costs patients less money and possibly grants them a greater quality of life with a possibility fewer side effects.

And why am I seething? That sounds great!

  • a) It’s the same damn company comparing two similar drugs that it manufactures,
  • b) both are laden with possible shit-tastic side effects,
  • c) both can only be taken for a minimum amount of time , and
  • d)…the best for last: San Diego’s own Dr. Agarwal is listed as an author, a consultant for Abbvie’s research, and he helped with the “inception, design, and analysis” of this study. The same Dr. Agarwal who accepted $315,000 from Abbvie from 2013-2017. And I’ve been told my many of his Endo patients that he often pushes Lupron and Elagolix for treatments.

Does it make me want to consider taking Elagolix to manage my Endo pain? Not one bit.

I was on Lupron for six months and it was one of the hardest things I’ve ever done, physically and mentally. Many people I’ve talked to had horrendous side effects and continued to have them long after quitting the treatments. And ABC 10 News interviewed several of our local EndoSisters about their Lupron experiences. It’s my understanding that Elagolix is very similar to Lupron…so I’ve zero desire to put my mind and body through such torture again…for a temporary, limited-use band-aid drug. But, I will always say this: don’t let my opinion sway you from a treatment option.

A fellow EndoSister, Magda, has a different perspective and she has given me permission to share her words today:

“I had a very good experience meeting with Dr A a few months ago finally so I don’t agree with a lot of the comments made about him. 

“I’m on a different study, for [redacted] which is similar but not one he is associated with and he thanked me for doing so even, and honestly my endo pain surprisingly enough I feel is quite nonexistent at this point, around 8 weeks in on non-placebo drug. Obviously if some saw me in a walker this last weekend it’s bc I need surgery on my hip from the labral tear because of a car accident but I’m beyond grateful that my endo is finally under control with one of the newest drugs out there for it, and with the addback therapy I haven’t seen any real side effects I’ve noted. In 2 weeks I’ll have my bone density rechecked so we can see where that is but I feel grateful to finally be on something helping control my endo pain, especially with limited side effects. 

“Since surgery is clearly not an end all option for our disease we’ve all learned maybe we should keep an open mind that there are some doctors out there that are truly trying to actually find a solution to at least help control our daily symptoms and in my opinion that is what Dr A is doing with his current practices, as a cure is not that simple. Unfortunately most diseases don’t have a cure, all kind of people take daily meds for all kind of things, like high blood pressure, diabetes, thyroid problems, high cholesterol, migraines, I could go on and on and on……trust me I get it. I literally cried my eyes out earlier this year the first day a doctor told me I was in denial that I had endometriosis and needed to be doing something about it, but mainly because I realized she was right. I also realized there are a lot worse things in life and in some case way worse conditions, especially some that don’t have a few pills that can help lower the pain levels or even possibly not help you in staying alive.

“So I count my blessings that I finally know what’s caused my pain, even though it took a long 21 painful years and a horrendous almost near death experience in the hospital last year just to get a diagnosis and finally know, but at least now I know and I’m doing something about it.

“That’s why I joined a study. To help not only myself but all the countless women who might still not know, and especially the children, more specifically the ones in my family that might be the unlucky ones to get this disease as well…..everyone has their own choices to make in life. I’ve made mine to help make a difference in any way I can. My question is what are you doing to help. If not others, at least for yourself. God put doctors and scientists on this earth to work on and help possibly eventually find cures, or at least medications that can help, that’s what the current studies out there are for. Without patients willing to help test the products, they will not be able to help us. And who knows, maybe you will actually feel better in the process. I know I do. And I at least have that to be grateful for. That’s my food for thought on this topic. “

Please, please, PLEASE do your own research and know what you’re getting into first: read the entire FDA drug pamphlets, analyze the studies, talk to others that have tried it, and question your healthcare providers. Most importantly: trust your gut. The decision is yours, and yours alone.

Resources:

Future Medicine – (Article, Feb. 2019) Cost–effectiveness of elagolix versus leuprolide acetate for treating moderate-to-severe endometriosis pain in the USA

ABC 10 News Interviewed Local EndoWarriors About Lupron Depot

Stillframe from ABC10 story about San Diego Endosisters who speak about about Lupron Depot

Jennifer Kastner of ABC 10 News San Diego reached out to Bloomin’ Uterus to see if we had any of our local Endo Warriors that had treated with Lupron Depot. Several of us had and jumped at the chance to share our experiences on the drug.

Five EndoSisters, Jennifer, and her cameraman Adam met for a two-hour interview one afternoon early this year. It was an incredible experience. We each had the opportunity to share our Endometriosis stories and our experiences on Lupron Depot.

One Sister has chosen not to take Lupron and talked about her battle with physicians to respect that decision.

The 2-hour Q&A session was paired down to a 5-minute investigative report. Jennifer did a wonderful job of fitting in a bit of our stories, as well as covering the side effects of Lupron, and the havoc it can cause.

If you’d like to watch the interview and read the more in-depth written report, please check out ABC 10 News’ page.

I’m grateful to Jennifer and Adam for reaching out to us and dedicating their afternoon to our interviews and for their weeks of investigative research. And I’m so proud of, and equally grateful to, our EndoWarriors who were able to join me that day: Melinda, Amanda, Brooklyn, and Linda – I love you. And am so pleased that you’re a part of my life.

Thank you for all that you do. Together we can achieve great things!

Orilissa: AbbVie’s New Drug to Manage Endometriosis Symptoms

Screenshot of FDA Drug Label for Orilssa
Screenshot of FDA Drug Label for Orilissa, July 24, 2018

You may have seen news articles and press releases flying around the Internet since yesterday regarding a new drug released to manage Endometriosis pain.  I wanted to share this with you because, although I’ve no intention of taking the drug myself, I know that it may help women who suffer. And it may help better educate you on your decision.

I’ve been following it for a while and you can read my thoughts about AbbVie’s SpeakEndo commercials and website, as well as their expedited application for FDA approval, and the track records of other drugs that have done the same.  And according to Business Insider, Orilissa may cost approximately $850 per month, or roughly $10,000 per year for prescriptions (I’m assuming those figures are calculated without health insurance).  Orilissa is estimated to hit markets for prescriptions in August of this year.

So, here you go:

On July 23, 2018, the Food & Drug Administration approved AbbVie’s new drug to treat Endometriosis pain. You may have seen it referred to as Elagolix, but it has been officially named Orilissa. It is an oral GnRH antagonist.

Please do your own thorough research before talking to your physician.

In the Resources section below is a link to the FDA’s drug fact sheet, which includes a .pdf of the pamphlet that should come with the drug. Read it. Review the clinical trials. And decide for yourself.   You can read the .pdf which I have downloaded, or by accessing the FDA’s site and downloading it for yourself.

It appears it has limited allowable dosing (6 months to 2 years), may cause liver issues, may cause bone loss, may cause depression and suicidal thoughts, and may interact with hormonal birth control. Some adverse reactions during clinical trials included appendicitis, abdominal pain, back pain, hot flashes, night sweats, nausea, decreased bone mass density, headache, insomnia, mood swings, depression, lack of a period, anxiety, joint pain, decreased libido, diarrhea, weight gain, dizziness, constipation, and irritability.

One participant in the clinical trials committed suicide two days after she stopped treating with the pill. She was 44 years old, had treated for one month, and had no medical history or life stressors that would have been indicative of suicidal thoughts.

Where did I get all this info? The FDA drug pamphlet.

Don’t trust me, read it for yourself.

Weigh the pros and cons.

And talk to your doctor.

A February 2019 study showed that women in Phase 3 Trials of Elagolix had improved period pain and non-period pelvic pain than those who were given the placebo pill. It stated that most adverse events were mild to moderate, but there was a risk of bone loss among patients.

And a June 2019 study showed that women in a 6-month clinical trial that were given Orilissa were at work 2-4 hours longer per week than women who were given the placebo, improving their attendance.

We are our best advocate. Do what you feel is best for you. But, please, do it informed and do it safely.

Knowing how poorly my body handled Lupron Depot (another AbbVie product that is incredibly similar), and how I became so severely depressed and suicidal on it, I will never again subject my body to something similar.  It did nothing in the long-term to stem my Endometriosis.  And was an incredibly difficult journey while on Lupron, as well as a long while before my body cleared itself of any side effects.  That is why I choose not to take Orilissa.  The decision is an individual one.  Never again.  But, again, I will never tell you not to try something; it may very well help you cope with your symptoms.  Understand, though, that it is a band-aid.  It will mask your symptoms; not clear your body of Endometriosis.  I learned that one the hard way…

If you do your research and make a well-informed decision to start (or not start) Orilissa, I wish you all the best of luck and health.  There are no judgments here.  Only well-wishes.

And, if you wish to see a quick snapshot of the participants and findings of the two clinical trials, please visit this FDA page.

**Updated June 25, 2019**

Resources:

AbbVie – (July 24, 2018; Press Release) AbbVie Receives US FDA Approval of Orilissa (elagolix) for the Management of Moderate to Severe Pain Associated with Endometriosis

Business Insider (July 24, 2018; Article) A New Treatment for a Condition that Can Feel Like Tiny People Skating on Razor Blades in Your Stomach and Affects an Estimated 200 Million Women Just Got Approved

Drugs & Therapy Perspective (Feb. 2019; Abstract) Elagolix in Endometriosis-Related Pain: a Profile of its Use and Approved in the USA

Fertility & Sterility (June 2019; Abstract) Impact of elagolix on work loss due to endometriosis-associated pain: estimates based on the results of two phase III clinical trials

US Food & Drug Administration – Drug Database: Orilissa

~ 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.

Questions re: Hormone Therapy & Endo

For those of you who have Endometriosis or know someone who does, Bloomin’ Uterus and The Pharmacists Clinic will be hosting a workshop about hormonal therapy and Endometriosis on August 31st. Even if you cannot attend the event : If you have questions about any hormonal therapy, whether it be birth control pills, IUDs, implants, Lupron Depot, Letrozole, Depo Provera, or others, please feel free to email Dr. Raffie at drrafie@pharmacistsclinic.com. She will do her best to address the question in the presentation. We’ll be taking detailed notes and will write a post-event summary, too. And if you’re in the San Diego area and are interested in attending the event, let me know. I can send you more info.

Hormonal Therapy & Endo Workshop

320px-Opened_Oral_Birth_Control

August 31, 2016, from 6:00pm-7:00pm (you can arrive as early as 5:45pm)

Mission Valley Library; Seminar Room A; 2123 Fenton Pkwy, San Diego, CA 92108

Join us to discuss Endometriosis treatment options with clinical pharmacist, Dr. Sally Rafie. Our focus will be on hormonal therapy, such as hormonal birth control and other hormone regulators. We will review effectiveness, side effects, and common concerns.

The talk will be interactive and casual, so please send in your questions in advance (to drrafie@pharmacistsclinic.com) or bring them with you!

Speaker:

rafie
Dr. Sally Rafie, PharmD, BCPS
The Pharmacists Clinic
www.pharmacistsclinic.com
www.instagram.com/pharmclinic
www.facebook.com/pharmacistsclinic

IMPORTANT: seating is severely limited. As of this moment, there are only 9 seats available.  If you RSVP and need to cancel, please let me know so I may review the waiting list. You will receive a confirming message from me that you are on the seating list, as well as my telephone number.  You can either RSVP on our Facebook event page https://www.facebook.com/events/1022030877903809/ or by emailing me directly at lisa@bloominuterus.com.

We would like to thank Dr. Rafie and Sama for all of their help in coordinating this event.