Saturday, 1 August 2015

Macitentan (Opsumit)

I have serveral concerns in taking my first 30mg dose.  It's usually taken at 10mg every day for a year.  Not on and off at higher doses.  This study made me feel quite a bit better:
32 healthy subjects took up to 30mg for 10 days without any side effects.

The second concern is that I want to go up to 60mg/day.  This is a link to the prescribing information which mentions going to 600mg and getting liver damage.  It also says there is data on its use with sildenafil. 


My first day went well at 30mg.  The only side effects are actually positive.  This drug does do a great job at making it easier to breath.  I don't have any problems.  I do walk aggressively every morning and noticed I'm hardly breathing up the hills pushing my 65lb sled.  I think I started getting some chest pains, so I stopped and breathed a little harder.  It went away immediately.  It made me drowsy, but not bad.  I slept well for the first time in weeks.  I'd say it counter-acted the dex nicely in this regard.  We'll see how the higher doses go.  I'm on 40mg now.


-Seth

31 comments:

  1. I thought I'd re-post this for people interested in obtaining Macitentan.

    Katja just informed me that its likely the Russian internet source is not good at 600 EU. It might be a sham. She just got another quote that is closer to 4000. I know that it is available in Germany and Canada. I talked to Farmacia Especializadas in Tijuana. They say they can get it out of Mexico City in two days and they don't require a prescription at the physical pharmacy. I don't know about on line. They have a website: www.farmaciaespecializada.com.
    018007155150. Another person on the forum just recently went down to another boarder town looking and was told it wouldn’t be available for another 6 months or so. So you might want to call or email my source in Mexico. I can see on their website that they have sales offices in Mexico and Russia. -Seth

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  2. Day 3 at 50mg went too drowsy. So I didn't go up to 60mg on day 4 as planned. I stayed at 50mg for 4 days then went to 30mg on my last of 7 days. Sleeping too much - 18 hours/day. Blood pressure is still fine. Today is day 4 on my 7 day part of the off cycle and I am still sleeping 10hours/day. I have still been able to do my 45 minute walk every day and am feeling mentally good. I am considering only doing 30mg/day on my next 7 days on temodar.
    -Seth

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  3. September 14, 2015
    Sorry to leave the forum for awhile. I've had a tough time here.I went to 50mg anyway for the next 7 days on. It just about did me in!! I slept for about 9 days straight and couldn’t work out, lost 20 pounds. But at least I gave stopping the progression my best shot (I have also been on my full cocktail). The subsequent MRI showed growth, however. 27 to 32mm with a little new swelling. Now I am resting after 7 days on 30mg (2nd chomo round). This is much easier to recover from, just a couple of days of sleeping.
    I have my next MRI in 10 days or so. Hopefully there will be no growth and I can continue on my cocktail. But my NO is getting very nervous with me being unmethylated and staying on temodar knowing it isn’t supposed to work. He wants it resected and to put me on CCNU+ Avistan. I don’t want to do the Avistan right now. Any thoughts??

    Also wanted to know if anyone has heard of using other ERAs instead of macitentan like Ambrisentan or Bosentan. In the pulmonary field they are considered pretty much the same and much more available.

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  4. Seth,
    Thanks for sharing your experimentation with macitentan. This is very valuable information as you are the first person I know of to add this to their cocktail.

    Sorry to hear about the progression. Have you considered adding Keppra and/or disulfiram and/or fluoxetine (Prozac)? These have all been shown (in vitro, in vivo) to inhibit MGMT thus sensitizing resistant glioma cells/tumors to TMZ.

    CCNU is pretty ineffective for MGMT-unmethylated tumors, but the same sensitization via Prozac, Keppra etc. should apply to CCNU as CCNU-mediated DNA damage is also repaired by MGMT. Anyhow, the CCNU+Avastin combo was only moderately effective for unmethylated tumors. I've seen better results with metronomic TMZ. Do you know anything about your tumor's EGFR status? This should really be routine testing for all GBMs.

    As for your question on other ERAs, the mouse study that combined macitentan with TMZ stated this:

    "In a phase 2 trial in patients with stage IV melanoma, the combination of
    the dual endothelin receptor antagonist, bosentan, with dacarbazine therapy had no
    effect on tumor progression (50). In comparison to bosentan, macitentan has a
    significantly lower dissociation rate and a 15-fold greater receptor occupancy half-life, which results in increased potency and sustained target blockade."

    Thus macitentan may have superior pharmacodynamics compared to other drugs like bosentan.

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  5. Hi Seth,
    good to hear from you again.
    I really hope your next MRI shows no growth.
    My dad gets his MRI in a couple of days, but he needs to wait 8 days for the results.
    Good luck, Lycka

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  6. Hi Stephen. Thank you so much for the input/suggestions. I am, and was on metforim, keppra, disulfiram, minocycline, celebrex, sildenafil, Prozac, and Tagamet during these last two chemo cycles. I was very torn with whether or not to go with the metronomic cycle to begin with knowing it works well with unmethylated tumors. But I thought that MD Anderson might know something about the 7 days on and 7 days off regime that works better with the higher dosing of the macitentan as they are using that in all their clinical trials. So now I know for me, I need the 7 days off to recover from the 7 days on the macitentan and I also know that this high dose stuff is not palatable for me. I don’t want my face planted in my pillow ½ the time. So if I have a chance to go another TMZ cycle, its going to be metronomic using 10mg with my cocktail. (I believe this was your initial hunch when someone asked you a couple months ago) I don’t know how MDA is going to manage their clinicals going on the high dose macitentan for the 7 days on and the 7 days off. They must be giving stimulants to keep their patients awake. I can’t imagine…
    My NO refuses to test for EGFR status. I’ll keep hammering away with him about it. Right now I am focused on the Novacure with him. All I need is for him is to write me a prescription and I can get it according to Optune.
    -Seth

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  7. Seth, how do you afford macitentan, when it seems that the standard price is over $7000 for 30 pills of 10 mg each?

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    1. It is insanely expensive. Fortunately I was able to get some serious support from friends a family to try this. I paid $3200 for 30 pills out of Germany. We will see if it pays off. The results for my next MRI are in on Wednesday.

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  8. The price in Canada is about $4000 in a regular pharmacy not online.

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  9. Wow. That's insanely expensive..

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  10. Goods news guys!! No growth on my last MRI!!!! My NO was surprised. He squared off and looked me in the eye and asked if I had upped my dex to 4mg for the MRI. "You didn't change anything else"? He was convinced we were going into surgery this week. I still have some swelling still so I am still on 2mg of dex. Our next goal is to get off the dex.
    I am day three into my third chemo cycle. It's metronomic with 10mg of macitentan, the cocktail, and the supplements. So far its much more tolerable than doing the 30mg, 7 days on and 7 days off. We will see how I feel in a couple of weeks. Thanks again everyone, Stephen especially, for your support. I am absolutely convinced that today would have had a different outcome without this forum.

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    1. Fantastic news Seth. We all rejoice in your victory.

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    2. I am so happy for you Seth!
      Before your Last MRI was made, were you on metronomic TMZ schedule? How many mg's are you taking?
      Thank you a lot.
      -Lycka

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    4. Great news !
      Thank you for sharing, give us a lot of hope.

      Melinda

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    5. Did you change your cocktail meds between the 2 MRI's? May I ask you what te pharmacy is called where you buy the macitentan? Thank You

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    6. Seth,

      This is awesome! Keep crushing it!

      Kendall

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  11. I'm so glad to hear this Seth!! I love hearing stories like this, when the docs are surprised at how well people are doing, sometimes not even knowing about the cocktails people are on ;)

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  12. I forgot to mention a rather important detail. The macitentan can seemingly suck the electrolytes almost completely out of you without warning. If you have an arrhythmia, this can be serious. I thought that because I was going from 30 to 10mg/day I was going to have an easier time. Not so. I was over 110 bpm and blood pressure at 94/54. 15 minutes into it my heart goes into synced multi-nodal firing. My wife is jamming ice water, salt water, and electrolytes down me until I think I'm going to float away. 5 minutes later the multi-nodal firing is subsiding and I'm down to 90bpm with my blood pressure stabilizing. It took another 30 minutes for things to reasonably stabilize. During all of this, I made it clear not to call 911 or I'm going to end up in the hospital with a bunch of dex being shoved down me after which comes the treadmill torture with all the electrodes. That can take weeks to pull out of.
    So if you have an arrhythmia, know your disease before you try macitentan. I was prepared with ice water, salt water, electrolytes, blood pressure monitor and stethoscope. I have a rather mild arrhythmia and this was my 3rd scary episode. The last one happened over 15 years ago. So this surprised me.

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  13. Hi Lycka,
    The only change between the 2 MRI's in my cocktail was a minor increase in THC before bedtime. I've been ramping it up as I figure out how to tolerate it. The bottle says "Endocann, balanced, 5 25mg soft jell caps. Now I am taking 1/2 a jell cap (kind of messy).
    I'll try to make the chronology clear of the dosing. Sorry its so confusing. First came the baseline MRI that shows profession through chemoradiation
    Then I I went 7 days on, 7 days off, then 7 days back on and 7 days off 50mg of macitentan and 140mg of temodar. MRI still shows growth.
    Then came 7 days on, 7 days off,and again 7 days on and 7 days off of 30mg of macitentan and 140mg of temodar which brings us to the current MRI showing no growth. I have now changed, yet again, to a metronomic schedule consisting of 10mg of macitentan and 40mg of temodar daily.

    I don't know what pharmacy I got the macitentan out of in Germany. It was all a rather convoluted ordeal that was spear headed by two friends who were over there for the summer. I was very blessed to have the support of them and their contacts to get the macitentan. I don't know that this was a repeatable process. I am sort of waiting for the macitentan to be available from Mexico here in the next couple of months to stock up again.
    Yes Stephen, it was quite the victory for me especially after having to endure comments like,"that's just a fad. I've had patients try that and they are all dead".

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  14. Yet another update, my wife was picking through the last MRI report and saw that the tumor actually shrank from 3.4cm to 2.2 cm in the sagital plane.Somehow my NO overlooked this incredible news.

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  15. Seth, that's fantastic news. Thanks for the update.

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  16. my last MRI brought bad news. All my work was undone and then some. my tumor grew to 36mm. The enhancement continued to fade out which my NO dismissed as being not relevant . So 10mg with metronomic temodar didn't work for me. I suppose that perhaps it was never the macitentan that ever wrked but the bad side effects that caused me to loose 20 plus pounds as I understand that in and of itself can be very effective. so now its a race to surgery and a change from temodar to CCNU. Darn, darn, darn it. looking at clinical trials. any suggestions? I am in So Cal.

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    1. Seth, Sorry to hear that your last MRI brought bad news, but it's heartening to know that surgery is still an option.
      Keep up the fight.

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    2. Thanks LInda. It's good to be reminded that I still have good options available . I had so mudh invested emotionally and financially in this direction that this news was quite devastating. Alll these ups and downs are also getting to me. Gut I'll settle down in a double of days and regroup to find some good clinical options and another good direction to take.

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    3. Hi Seth,
      I know exactly what you mean, we put so much into our treatment cocktail, all our energies and time, plus the financial costs, and emotional stress not to mention feeling like crap when swallowing bucket loads of tablets and swilling down foul tasting herbal concoctions all the while keeping a positive attitude and being so hopeful throughout that when an MRI like yours comes back it is just gut wrenching. Good luck , hopefully next MRI will kick ass

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  17. I'm also sorry to hear this news Seth. But I like your attitude - regroup, look at clinical trials, stay proactive.

    There are a number of interesting trials in your part of the country for recurrent GBM: allogeneic lysate DC vaccine at Cedars-Sinai, the SL-701 vaccine at Cedars and UCLA, Toca511 at UCLA and UCSD.

    http://astrocytomaoptions.com/currently-recruiting-trials/

    Wishing you the best in finding another good direction.

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