Recognition by the US Food and Drug Administration (FDA) that RLX030 has the potential to address a serious unmet medical need

If approved, RLX030 has the potential to be the first treatment breakthrough for Acute Heart Failure patients in 20 years

RLX030 is the second Breakthrough Therapy designation by the FDA for Novartis investigational treatments, following LDK378

Basel, June 21, 2013 – Novartis announced today that the US Food and Drug Administration (FDA) has granted Breakthrough Therapy designation status to RLX030 (serelaxin), an investigational treatment for patients with acute heart failure (AHF). The FDA has concluded that RLX030 qualifies for a Breakthrough Therapy designation after considering the available clinical evidence which supports a substantial improvement over currently available therapies for AHF[3], a life-threatening illness…………….

http://www.pharmalive.com/novartis-serelaxin-gets-fda-breakthrough-designation

Serelaxin (RLX030) is an investigational drug targeting the relaxin receptor. Serelaxin is a recombinant form of human relaxin-2, a hormone that (among other functions) is produced during pregnancy and mediates the haemodynamic changes that occur during this time , such as increased blood output of the heart and blood flow in the kidney.

Serelaxin is currently undergoing clinical trials in patients with acute heart failure, and is being developed by Novartis.

structure

L-Serine, L-α-aspartyl-L-seryl-L-tryptophyl-L-methionyl-L-α-glutamyl-L-α-glutamyl-L-valylL-isoleucyl-L-lysyl-L-leucyl-L-cysteinylglycyl-L-arginyl-L-α-glutamyl-L-leucyl-L-valyl-L- arginyl-L-alanyl-L-glutaminyl-L-isoleucyl-L-alanyl-L-isoleucyl-L-cysteinylglycyl-L- methionyl-L-seryl-L-threonyl-L-tryptophyl-, cyclic (11→11′),(23→24′)-bis(disulfide) with 5-oxo-L-prolyl-L-leucyl-L-tyrosyl-L-seryl-L-alanyl-L-leucyl-L-alanyl-L-asparaginyl-L-lysyl-L- cysteinyl-L-cysteinyl-L-histidyl-L-valylglycyl-L-cysteinyl-L-threonyl-L-lysyl-L-arginyl-L- seryl-L-leucyl-L-alanyl-L-arginyl-L-phenylalanyl-L-cysteine cyclic (10’→15′)-disulfide

CHEMICAL NAMES

1. L-Serine, L-α-aspartyl-L-seryl-L-tryptophyl-L-methionyl-L-α-glutamyl-L-α-glutamyl-L-valyl-
L-isoleucyl-L-lysyl-L-leucyl-L-cysteinylglycyl-L-arginyl-L-α-glutamyl-L-leucyl-L-valyl-L-
arginyl-L-alanyl-L-glutaminyl-L-isoleucyl-L-alanyl-L-isoleucyl-L-cysteinylglycyl-L-
methionyl-L-seryl-L-threonyl-L-tryptophyl-, cyclic (11→11′),(23→24′)-bis(disulfide) with
5-oxo-L-prolyl-L-leucyl-L-tyrosyl-L-seryl-L-alanyl-L-leucyl-L-alanyl-L-asparaginyl-L-lysyl-L-
cysteinyl-L-cysteinyl-L-histidyl-L-valylglycyl-L-cysteinyl-L-threonyl-L-lysyl-L-arginyl-L-
seryl-L-leucyl-L-alanyl-L-arginyl-L-phenylalanyl-L-cysteine cyclic (10’→15′)-disulfide

2. Human relaxin 2 (relaxin H2)

MOLECULAR FORMULA C256H408N74O74S8

MOLECULAR WEIGHT 5.96 kDa

SPONSOR Novartis Pharma AG

CODE DESIGNATION RLX030

CAS REGISTRY NUMBER 99489-94-8

Treatment of acute heart failure

Structure

http://www.ama-assn.org/resources/doc/usan/serelaxin.pdf

1. H. Spreitzer (4 March 2013). “Neue Wirkstoffe – Serelaxin”. Österreichische Apothekerzeitung (in German) (5/2013): 36.
2.  Dirk Einecke (23 November 2012). “Schwangerschaftshormon gegen Herzschwäche” [Pregnancy hormone against heart failure]. ÄrzteZeitung.
3.  Conrad KP (August 2011). “Maternal vasodilation in pregnancy: the emerging role of relaxin”. Am. J. Physiol. Regul. Integr. Comp. Physiol. 301 (2): R267–75. doi:10.1152/ajpregu.00156.2011. PMC 3154715. PMID 21613576.
4.  Teerlink, John R; Cotter, Gad; Davison, Beth A; Felker, G Michael; Filippatos, Gerasimos; Greenberg, Barry H; Ponikowski, Piotr; Unemori, Elaine; Voors, Adriaan A; Adams, Kirkwood F; Dorobantu, Maria I; Grinfeld, Liliana R; Jondeau, Guillaume; Marmor, Alon; Masip, Josep; Pang, Peter S; Werdan, Karl; Teichman, Sam L; Trapani, Angelo; Bush, Christopher A; Saini, Rajnish; Schumacher, Christoph; Severin, Thomas M; Metra, Marco (1 November 2012). “Serelaxin, recombinant human relaxin-2, for treatment of acute heart failure (RELAX-AHF): a randomised, placebo-controlled trial”. The Lancet.doi:10.1016/S0140-6736(12)61855-8.