Wednesday, December 28, 2016

New kids on the Block – What has become of the Emerging Therapies Five Years later?




Just before the 2011 ACR Annual Meeting in Chicago, I had written about emerging therapies in rheumatology based on the 2011 EULAR Annual Meeting in London. I just wondered, what has happened to those therapies, DMARDs, biologics etc.

1. Biosimilars
After the studies.it took some time, but now we have Celltrion’s infliximab, then called CT-P10. In the U.S: it’s marketed as Inflectra®, in Germany for instance as Remsima® by Mundipharma and Inflectra® by Hospira (bioidenticals!). Flixabi® by Biogen is approved in the EU.
In the EU we also have Benepali by Biogen (joint venture with Samsung), which is an etanercept biosimilar. Erelzi® by Sandoz has been approved as an etanercept biosimilar by the FDA.

2. Anti-CD-20 Monoclonal Antibody (like Rituximab)
Not much has happened, when it comes to new Anti-CD-20 Monoclonal Antibodies. Ocrelizumab has been recently studied to treat multiple sclerosis. I have concerns when it comes to ocrelizumab and other second generation B-cell depleting agents. For more details refer to links.

3. Co-Stimulation-Inhibition goes subcutaneously
Abatacept SC is well established, but patients having started on IV tend to go back to IV if switched to SC (own observation, applies to tocilizumab as well).

4. Anti-Interleukin-6 Monoclonal Antibody (like Tocilizumab)
At the 2016 ACR Annual Meeting we heard about a new anti-IL6 MAB: gerilimzumab. “Gerilimzumab is a humanized llama antibody with femtomolar potency and a Fc region mutation engineered to prolong halflife.” (Abstract #1607). Alan Glicklich and colleagues presented a phase 1 study.
Sirukumab has been submitted for approval both in the EU and the US. For more details refer to links.
ALX-0061 has been named: Vobarilizumab. The question if a phase 3 study will really start is still unanswered. For more details refer to links.

5. Anti-BAFF Monoclonal Antibody
Belimumab, an anti-BAFF MAB, has been approved for the treatment of SLE.
T Dörner and colleagues presented the following study [#3033]: “Safety and efficacy of single dose VAY736 (anti-BAFFR mAb) in patients with primary Sjögren’s syndrome (pSS)”. “VAY736 is a novel, defucosylated, human IgG1 mAb targeting the receptor for B cell activating Factor of the TNF family (BAFF-R), providing both enhanced antibody-dependent cellular cytotoxicity-mediated depletion of B cells and blockade of BAFF:BAFF-R signaling that drives B cell differentiation, proliferation and survival.” Conclusion: “Despite a limited, single infusion, VAY736 achieved in this early phase trial trends for improvement in the primary outcome and across all secondary outcomes. Thus, this treatment was safe and suggests a positive therapeutic effect for this dual mechanisms of action in pSS that warrant further evaluation.” Which means, we’ll have to wait another five years.
Nothing on LY2127399 or tabalumab as it has been named.

6. Anti-Lymphotoxin-alpha Monoclonal Antibody
I had written about MLTA3698A, a lymphotoxin-alpha MAB, which has later been renamed to pateclizumab. Lymphotoxin-alpha is also known as tumor necrosis factor-beta (TNF-β). In 2013 I had to ask, if pateclizumab had been abandoned silently. My latest evaluation ended: “The story of pateclizumab ends here. A dead end.

7. Secukinumab (an Anti-IL17a Monoclonal Antibody)
In the meantime secukinumab has come to the market as Cosentyx®, which I’ve used already.
There have been recent studies on ABT-122, a novel dual-variable domain immunoglobulin (DVD-IgTM), which targets both TNF alpha and IL17a.

8. Oral JAK-Inhibitor, “small molecules”, SYK-Inhibitor and others
Xeljanz® (tofacitinib) has been approved in the US. EMA has accepted for review the Marketing Authorization Application (MAA) Xeljanz® (tofacitinib). But this has happened nine months ago.
The Committee for Medicinal Products for Human Use (CHMP), which belongs to EMA,  adopted a positive opinion, recommending the marketing authorization for Olumiant® (baricitinib) for the treatment of rheumatoid arthritis.
Let’s see, who comes first. The oral JAK-Inhibitor Tofacitinib seems to be the most promising agent.

Links:


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