Arrowhead Pharmaceuticals, Inc.

Aaron Almeida

David B Rozema

Darren H Wakefield

Andrei V Blokhin

Jeffrey Carlson

David L Lewis

Steven B Kanner

Lauren Almeida

Anthony Nicholas

Jonathan D Benson

Tao Pei

Zhen Li

So Wong

Weijun Cheng

Justin Woods

Vladimir S Trubetskoy

Agnieszka Glebocka

Erik W Bush

Matthew Fowler-Watters

Stacey Melquist

Lauren J Almeida

Angieszka Glebocka

Integrin ligands having serum stability and affinity for αvβ6 integrins are described. Compositions comprising αvβ6 integrin ligands having serum stability and having affinity for αvβ6 integrins and methods of using them are also described.

Alpha-v beta-6 integrin ligands and uses thereof

RNA interference (RNAi) triggers and RNAi trigger conjugates for inhibiting the expression of Hif2&#x3b1; (EPAS1) gene are described. Pharmaceutical compositions comprising one or more Hif2&#x3b1; RNAi triggers optionally with one or more additional therapeutics are also described. Delivery of the described Hif2&#x3b1; RNAi triggers to tumor cells in vivo provides for inhibition of Hif2&#x3b1; gene expression and treatment of cancer.

Compositions and methods for inhibiting gene expression of Hif2alpha

Integrin ligands having serum stability and affinity for &#x3b1;v&#x3b2;6 integrins are described. Compositions comprising &#x3b1;v&#x3b2;6 integrin ligands having serum stability and having affinity for &#x3b1;v&#x3b2;6 integrins and methods of using them are also described.

RNA interference (RNAi) agents and RNAi agent conjugates for inhibiting the expression of the LPA (apo(a)) gene are described. Pharmaceutical compositions comprising one or more LPA RNAi agents optionally with one or more additional therapeutics are also described. Delivery of the described LPA RNAi agents to liver cells in vivo provides for inhibition of LPA gene expression and treatment of cardiovascular and cardiovascular-related diseases.

Compositions and methods for inhibiting gene expression of LPA

Described are improved disulfide-containing alkyne linking agents having have branched disulfides. The improved linking agents exhibit improved stability. The linking agents are useful for attachment of oligonucleotides to targeting groups or delivery agents.

Disulfide-containing alkyne linking agents

The present invention is directed compositions for delivery of RNA interference (RNAi) triggers to integrin positive tumor cells in vivo. The compositions comprise RGD ligand-targeted amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or conjugate) are further covalently linked to an RNAi trigger.

Polyconjugates for delivery of RNAi triggers to tumor cells in vivo

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Madison, WI, United States of America

Aaron Almeida