Nektar Therapeutics

C Simone Jude-Fishburn

Jennifer A Riggs-Sauthier

Timothy A Riley

Guy Lalonde

Hema Gursahani

Laurie A VanderVeen

Mei-chang Kuo

Mary J Bossard

Tacey Viegas

Ping Zhang

David Lechuga-Ballesteros

Michael A Eldon

Harold Zappe

Yujun Wang

Xiaofeng Liu

Dennis G Fry

Dawei Sheng

Cherie F Ali

Chester Leach

Yuan Song

Haim Moskowitz

Christine Taylor Brew

Steven O Roczniak

Myong Gyong Lee

Elizabeth Louise Minamitani

Christine Brew

Elizabeth Minamitani

Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchioalveolar lavage followed by assaying residual lung material.

Chemically modified small molecules

The invention provides various methods comprising the administration of a CYP2D6 bioactive drug covalently bound to a water-soluble oligomer. Metabolism of CYP2D6 bioactive drug conjugates is diverted from CYP2D6 to alternative pathways, and the conjugates may therefore be utilized to alleviate the problems associated with interpopulation variation resulting from the genetic polymorphism in the CYP2D6 gene.

Methods of treating CYP2D6 alternative metabolizers

Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature.

Protease inhibitors having enhanced features

The invention provides peptides that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water-soluble oligomer.

Polymer conjugates of therapeutic peptides

The invention relates to (among other things) oligomer-cannabinoid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated cannabinoid compounds.

Oligomer-cannabinoid conjugates

Oligome-cannabinoid conjugates

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Redwood City, CA, United States of America

C Simone Jude-Fishburn