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Promising New Drugs For Myeloma: Will The Future Come Soon Enough?

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Published: Apr 15, 2011 10:04 am

Each year at the Annual Meeting of the American Society of He­ma­tol­ogy we hear about dozens of new drugs that are able to annihilate mul­ti­ple myeloma cells in the test tube and in animal models. Unfortunately, at the same meeting, we also sit through pre­sen­ta­tions and walk by posters of drugs that looked hot in the laboratory but then fail to work when given to real patients with myeloma.

This is not new. It has been the story with myeloma for ages. The myeloma cells are smart and are seemingly able to easily over­come any adversity that comes their way in the form of pesky new drugs. For those of us dealing with this dis­ease on a daily basis, we need some good news.

What are the most promising drugs to­day that can outsmart the myeloma cells? Will they work in patients who have failed other ther­a­pies? Will they have a reason­able safety profile?  Will a future filled with many active treat­ments and op­tions hap­pen soon enough?

If I were a patient with myeloma and none of the cur­rent treat­ments were work­ing for me, I would need to have at least some idea which drugs are the most promising, so that I could hunt for the best clin­i­cal trial. However, an Internet search turns up so many possibilities that it is hard for even trained hematologists to de­ter­mine the best op­tions among the array of clin­i­cal trials.

In this column, I will highlight drugs that are unquestionably active in myeloma. These are new treat­ments that are not com­mer­cially avail­able, but in my opinion clearly work in myeloma, even in patients who have failed other treat­ments. I will also discuss other promising drugs where the data sug­gest that there is at least a reason­able probability that they actually work in patients.

Note that by highlighting these drugs, my intention is not to sug­gest that the other agents being studied are unimportant. In fact, deciding the best treat­ment op­tion or a clin­i­cal trial for a given patient is a complex process that re­quires a great deal of thought and de­pends on many variables.

My goal is to simply in­form, and to illustrate the rationale for my hope and enthusiasm.

In the first category are com­­pounds that have shown clearcut ac­­tiv­ity in myeloma in terms of reducing mono­clonal (M)-protein levels by 50 per­cent or more when used on their own (single-agent ac­­tiv­ity). Of countless drugs that have been looked at and not yet approved for com­mer­cial use, only poma­lido­mide and car­filz­o­mib have shown sig­nif­i­cant single-agent ac­­tiv­ity in mul­ti­ple clin­i­cal trials. They seem to work in situations where other myeloma treat­ments have stopped work­ing. They are both in ad­vanced stages of devel­op­ment (i.e., Phase 3 trials are underway).

Pomalidomide: Pomalidomide (also called CC-4047) is a new immuno­modu­la­tory analogue of thalidomide (Thalomid) and Revlimid (lena­lido­mide). It was first studied by Schey and colleagues from the United Kingdom who treated 24 re­lapsed or re­frac­tory patients and found a re­sponse rate of 54 per­cent. Next, Lacy and colleagues at the Mayo Clinic tested the com­bi­na­tion of poma­lido­mide with low dose dexamethasone (Decadron) and showed ef­fi­cacy in re­lapsed dis­ease, in patients who had failed Revlimid and in patients who had failed both Revlimid and Velcade (bor­tez­o­mib). These re­­sults have since been con­firmed by the Multiple Myeloma Re­search Consortium (MMRC) and by in­ves­ti­ga­tors from the Intergroupe Francophone du Myeloma (IFM). Side effects seem reason­able and similar to Revlimid. Clinical trials are on­go­ing around the world. I hope that poma­lido­mide is approved soon.

Carfilzomib: Carfilzomib is a new pro­te­a­some in­hib­i­tor. It has a dif­fer­en­t chemical structure than Velcade, the prototype pro­te­a­some in­hib­i­tor. In a series of clin­i­cal trials con­ducted by the MMRC, car­filz­o­mib pro­duced re­sponses in approx­i­mately 50 per­cent of patients with re­lapsed myeloma, in­clud­ing 15 per­cent who were re­frac­tory to Velcade. Carfilzomib is given in­tra­venously. It appears to be well tol­er­ated and has a lower risk of neu­rop­athy (pain or tingling in the extremities) com­pared with Velcade. As with poma­lido­mide, con­firmatory stud­ies are on­go­ing around the world, and I am hopeful that the drug will be approved soon.

In the second category are agents that have not shown clear single-agent ac­­tiv­ity in myeloma, but are promising nevertheless based on re­sponses seen when they were com­bined with other drugs.

The histone deacetylase in­hib­i­tors, Zolinza (vorinostat) and panobinostat (Farydak), have both shown ac­­tiv­ity when com­bined with Velcade. With these drugs, we have reports of patients with myeloma that was pro­gress­ing while re­ceiv­ing Velcade ther­apy that responded promptly upon the addi­tion or either Zolinza or panobinostat. Clinical trials with these agents also sug­gest that the re­sponse rate when used in com­bi­na­tion with Velcade is more than what we would ordinarily ex­pect to see with Velcade alone. Large trials are on­go­ing with these treat­ments, and we eagerly await the re­­sults of these trials to de­ter­mine the role and fate of these two drugs.

Another treat­ment in this category is the anti CS-1 anti­body, elotuzumab. The re­sponse rate with elotuzumab plus Revlimid and dexa­meth­a­sone (Rd) appears to be much higher than what would be ex­pected with Rd alone.

Other po­ten­tial drugs that could join this category are heat shock pro­tein in­hib­i­tors (e.g., KW-2478) and phosphoinositide 3-kinase path­way in­hib­i­tors (e.g., perifosine).

There is one other drug that does not fit well into either category listed above, but nevertheless is just as promising: MLN9708, an oral pro­te­a­some in­hib­i­tor. My enthusiasm for this agent stems from the fact that it is avail­able on clin­i­cal trials and that it belongs to a drug class that has already pro­duced two active agents, namely Velcade and car­filz­o­mib.

I raised some questions in the beginning. I think I answered the first three. The fourth (also stated in the title) was not meant to be rhetorical. I know for a fact that the many myeloma in­ves­ti­ga­tors work­ing on these trials under­stand the urgency of the situation. The com­pa­nies that make these com­­pounds recog­nize the need for speed and have been incredibly sup­port­ive. The myeloma field has shown the on­col­ogy world a path to drug devel­op­ment with 4 new drug ap­prov­als in the last 10 years. I am quite hopeful that for most myeloma patients, the future will indeed hap­pen soon enough.

Dr. S. Vincent Rajkumar is a pro­fessor of med­i­cine at the Mayo Clinic in Rochester, Minnesota. His re­search focuses on clin­i­cal, epidemiological, and laboratory re­search for myeloma and re­lated disorders.

Photo of Dr. S. Vincent Rajkumar, professor at the Mayo Clinic.
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17 Comments »

  • Mark said:

    Dr. Rajkumar,

    Good article on the current drugs in the pipeline and a sincere "Thank you" for your work in combating this disease. As a patient, I am disappointed that researchers spend so much time on drugs that at best give us temporary remissions. Why is more time not spent on improving Allo transplants, or something that could lead to longer remissions or even cure without long term use of these toxic drugs? More young patients are getting this disease. I am worried that the current trend in Myeloma seems to be increaded use of drugs that we do not know what the longer term side effects are.

    Sincerely,
    Mark

  • nicola said:

    ^^^^
    Here I am: 31, from Italy, diagnosed in June 2010 and now in remission.

  • Peter Parker said:

    Dr. Rajkumar, thank you again, that you write a column at the beacon. That's a great deal for us patients to get informed by a myeloma thought leader. Please allow me to share my thoughts: Unfortunately - at date - there are statistically about 20.000 patients dying from myeloma in the U.S. every year. For this patients new discoveries come too late. Even 2011 we have no real control and significant progress. We're not there at all.*

    Anyway, in your article from December 2010 you talked about combinations, that could be the way to a better control. You described that new class agents, that accompanies the older ones, are desperately needed. What are your opinions of the promising new class agents (Arry 520; MOR202; STA-9090; INK128; El101; MAGE-A3 vaccine etc.)? Best regards, Peter Parker

    *(Myeloma killed one of my dearest friends with 42 recently. A passed away from host-versus-gradt disease will going through an allo transplant. He had only 3 years with myeloma. Specialists said: We could do nothing for you.)

  • Thomas L. said:

    Dr. Rajkumar-, will the discovery of the genetic myeloma markup (Broad-Institut) help the myeloma research significantly? The experts from my research center talk about important progress in the discovery of the mechanism, that changes smoldering to active myeloma. Do you think, there could be a real breakthrough, that we will see in the nearest future? I must admit, that the news from the last events (ASH, ASCO, ASCR) and most of the studies has been disappointing for me, because the steps seem to be small and with refractory disease the new agents are lab heroes without relatively poor outcome in the relapse setting. When will the revolution start? Thank you, Thomas L.

  • MARY said:

    Dr. Rajkumar: thank you for the info and also for the time you give to this terrible disease. Could you please tell about any new trial after the sequence of the MM genome lest month?.
    Any hope coming from the monoclonal antibodies on the way?.
    Best.
    Mary

  • Lori Puente said:

    Dr. R, great article and I thank you for it. Many patients who are lucky enough to get into CR, while worth celebrating, are all to aware that the hurdle of eventual relapse therapies may indeed be in their future. I have long maintained that while the path is not clear, it is exciting and filled with dedicated researching physicians in conjunction with organizations like MMRC, IMF and pharmas who are working hard to find a treatment that will bring us to a new paradigm in treating Myeloma. Thank you for helping us to understand and realize the dogged dedication of more than a few in this pursuit.

  • ROSE BOLTON said:

    I'm also expecting news from the new discovery around myeloma genome. Thank you. Rose

  • S. Vincent Rajkumar said:

    Many investigators are continuing to pursue ways to improve allogeneic transplantation, through laboratory and clinical studies. Despite the recent disappointing results, the Bone Marrow Transplant - Clinical Trials Network (BMT-CTN) is continuing to work on a successor allogeneic stem cell transplant trial. Trying to improve allogeneic transplants and finding new drugs to target the disease are not mutually exclusive. I agree that we need to pursue both approaches.

    I fully agree that what we need the most are new classes of agents. Drugs like pomalidomide, carfilzomib, MLN 9708 are derivatives of drug classes that we already know to be effective. Since there are no good laboratory assays that consistently predict clinical activity, it is hard to predict the likely winners. We just have to wait for the clinical trials. Thankfully, numerous trials are ongoing, and Im hopeful we will find new classes. Part of the problem in myeloma is that unlike, say, chronic myeloid leukemia and the bcr-abl translocation, we do not have an equivalent, specific, disease causing genetic abnormality that we can target. Another problem is that myeloma itself is probably a mix of different diseases on a molecular level, collectively called by one name based on clinical features. So it is hard to go after with a uniform approach. We do have specific drugs being developed targeting specific cytogenetic subtypes based on the genetic translocation, eg., t4;14. At present, I am also optimistic about cyclin dependent kinase inhibitors since pathogenetically most cytogenetic subtypes of myeloma have over expression of various cyclins. There are a couple of others that look promising based on early clinical results. Of the antibodies, antibodies to CS-1 (elotuzumab), CD38, IL-6 (a new fully humanized version), are high on the list.

    The genetic roadmap that was published recently will be very helpful. But it will take time to sort through given the unbelievable amount of data contained in the sequencing. It is like the proverbial hunt for a needle in a haystack. It is a massive haystack, but thankfully lots of people are combing through it.

  • Jeffrey Marchant said:

    Dr. Rajkumar,
    Thank you for this article and all you've done for myeloma patients. I especially value your commentary "Treatment of Myeloma: Cure vs Control." I'm curious why CEP-18770 was not one of the potential promising new drugs you mentioned. It has been raised as one of a number of possible drugs & clinical trials that may be useful to me in the future.

  • S. Vincent Rajkumar said:

    Thanks for pointing that out. CEP-18770 is an oral proteasome inhibitor, and should indeed be in the promising list, and there is an open trial recruting patients in the US.

  • S. Vincent Rajkumar said:

    Clarification- CEP-18770 is orally active in animal models, but the current clinical trial uses an intravenous formulation.

  • DR K RAGHU said:

    Hai, it was good to read a summary of newer drugs for Myeloma.I am a practising hematologist in Coimbatore in South India and am proud of you Dr.Rajkumar, for your poineering work in myeloma. As you may be aware myeloma occurs atleast a decade earlier in Indian paients and we have huge numbers of cases with limited access to latest treatments.
    I have a question about Autologous SCT in myeloma, is it REALLY better than combination therapy in the bortezomib era? Keep up your good work, I heard you will be lecturing im Mumbai later his year. I hope to see you there.

  • Pamela Lewis said:

    I am an RN who worked in western medicine before, during and after Reagan turned our countries compassionate and available medical system into a for-profit, industrial, corporate affair totally at the mercy of big pharma. It used to be that doctors decided how to treat patients, now it seems that the insurance business people do. My beloved husband has advanced M.M. and everyone should watch the following video who has cancer.

    At least watch the 1st 10-30 minutes . . .

    http://vimeo.com/24821365 ["Burzynski: Cancer Is Serious Business"]

    ( 1 hour, 48 minutes )

  • Paula said:

    Pamela
    I have sen this video, are you suggesting this as a possibility for MM patients.?

    Dr Raghu, I was surprised of your comments on patients in India, I am taking curcumin and had much faith in that, until I read your comments, as they would be taking curcumin daily, and yet have myeloma a decade earlier.

  • Henry said:

    Hi Dr. Rajkumar,

    Comparing Pomalidomide, Carfilzomib and Perifosine.
    Which agent do you think can better extend the life of a colon cancer patient?

    Thank you,
    Henry

  • R.D.Bhardwaj said:

    Hi Dr. Rajkumar,

    Can you please share your views on drug under trial from vaxil of Isarael?

    Many thanks,

    R.D.Bhardwaj

  • bindu said:

    Dear Dr. Rajkumar,
    I am from Kochi, Kerala.My husband (age 52)is under treatment for multiple myeloma since 2006. He was responding for the treatments fairly well.Recently he is having pain in difeernt parts of the body and now his eye is also becoming smaller. Does it show any symptom that the disease is progressing. we have taken almost all the medicines like, bortinet, zondria, linaldidomide etc.is there any new treatment to control the disese. Hope you will send reply by e mail.
    thanking you