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Polymers as Drugs

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Book cover Polymer Therapeutics I

Part of the book series: Advances in Polymer Science ((POLYMER,volume 192))

Abstract

Polymeric drugs are defined as polymers that are active pharmaceutical ingredients, i.e., they are neither drug carriers nor prodrugs. In general, the underlying concept behind these therapeutic agents is the utilization of high molecular weight and functional characteristics of polymers to selectively recognize, sequester, and remove low molecular weight and macromolecular disease causing species in the intestinal fluid. The high molecular weight nature of these therapeutically relevant polymers makes them systemically non-absorbed, thus providing a number of advantages including long-term safety profiles over traditional small molecule drug products. Furthermore, multiple functional groups in the polymers incorporate polyvalent binding interactions that can result in pharmaceutical properties not found in small molecule drugs. This article summarizes some of the most recent efforts for the discovery and development of polymeric drugs that have proceeded from discovery phase to market place. Examples include sequestration of low molecular weight species such as bile acids, phosphate, and iron ions as well as polyvalent interactions to bind toxins, viruses, and bacteria as well as polymeric enzyme inhibitors and fat binders as anti-obesity agents. Furthermore, use of functional polymers to treat autoimmune disease and sickle cell anemia has been reviewed.

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Abbreviations

GI:

gastrointestinal

SAR:

structure-activity relationship

LDLc:

low-density lipoprotein cholesterol

HMG-CoA:

3-hydroxy-3-methyl glutaryl coenzyme A

BAS:

bile acid sequestrant

C. difficile:

Clostridium difficile

PA:

protective antigen

EF:

edema factor

LF:

lethal factor

Tyr:

tyrosine

Trp:

tryptophan

VAP:

viral attachment proteins

HA:

hemagglutinin

SA:

sialic acids

Kd:

dissociation constant

M:

molar

mM:

milli molar

pM:

pico molar

HIV:

human immune virus

MRSA:

methicillin-resistant Staphylococcus aureus

C. parvus:

Cryptosporadium parvum

VRE:

vancomycin-resistant Enterococi

ROMP:

ring opening metathesis polymerization

S. aureus:

Staphylococcus aureus

RA:

rheumatoid arthritis

MS:

multiple sclerosis

TNF-α:

tumor necrosis factor alpha

GA:

glatiramer acetate

MBP:

myelin basic protein

CNS:

central nervous system

FDA:

Food and Drug Administration

EAE:

experimental allergic Encephalomyelitis

TAG:

triacyl glycerides

PEO:

polyethylene oxide

PPO:

polypropylene oxide

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Authors and Affiliations

  1. Drug Discovery and Development, Genzyme Corporation, 153 Second Avenue, MA 02451, Waltham, USA

    Pradeep K. Dhal, S. Randall Holmes-Farley, Chad C. Huval & Thomas H. Jozefiak

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  1. Pradeep K. Dhal
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  2. S. Randall Holmes-Farley
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  3. Chad C. Huval
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  4. Thomas H. Jozefiak
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Correspondence to Pradeep K. Dhal .

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Ronit Satchi-Fainaro Ruth Duncan

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Dhal, P.K., Holmes-Farley, S.R., Huval, C.C., Jozefiak, T.H. Polymers as Drugs. In: Satchi-Fainaro, R., Duncan, R. (eds) Polymer Therapeutics I. Advances in Polymer Science, vol 192. Springer, Berlin, Heidelberg. https://doi.org/10.1007/12_020

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