PRECISION POLYMER

Medical Applications of PEG: Long-Acting Modification, Precision Linkers, and Nanodelivery

2026-10-23 · Case Study

Polyethylene glycol (PEG) is a hydrophilic polymer widely used in medicine. Its high water solubility, flexible chain structure, and diverse options for end-group modification make PEG and its derivatives useful as pharmaceutical excipients, for modifying drug molecules, and for constructing delivery carriers. Applications span small-molecule drugs, protein and peptide therapeutics, antibody–drug conjugates, and nucleic acid therapeutics. Selecting appropriate chain lengths, end groups, and linkages can modulate drug solubility, stability, behavior in vivo, and release.

PEG-related medicines have achieved substantial commercial scale. According to companies’ reported 2025 results, the PEGylated antibody fragment Cimzia generated net sales of EUR 1.954 billion; Trodelvy, an antibody–drug conjugate containing a PEG linker, generated sales of USD 1.397 billion; and Zilbrysq, a peptide drug containing a precision PEG24 linker, generated net sales of EUR 217 million, approximately three times its 2024 sales. These products demonstrate commercial applications of PEG in protein modification, peptide drug design, and ADC development. Its value extends beyond conventional modification for prolonged action to functional linkers of defined length.

China has also continued to make progress in PEG-related medicines and delivery formulations. Domestically developed products including peginterferon alfa-2b, PEGylated growth hormone, and polyethylene glycol loxenatide have been approved, demonstrating applications of PEG modification in long-acting protein and peptide drugs. In nucleic acid delivery, Yuxi Walvax’s COVID-19 mRNA vaccine received registration approval from China’s National Medical Products Administration (NMPA) in September 2026. These developments show that domestic PEG applications now encompass long-acting biologics and mRNA delivery formulations and are supporting the development and use of related functional materials and pharmaceutical excipients.

PEG takes different forms and serves different roles across applications. It may be used directly as a formulation excipient, covalently attached to an active molecule, or incorporated into delivery systems such as liposomes, lipid nanoparticles (LNPs), and hydrogels. Short PEG or oligoethylene glycol (OEG) of defined length can also serve as a linker or hydrophilic spacer between functional modules.

Current pharmaceutical applications of PEG fall into the following main categories:

The following tables summarize applications of PEG and OEG in approved medicines and delivery formulations in China and internationally. They present representative products, their PEG or OEG structures, and their main functions, together with updates on selected investigational programs.

Table 1 Representative Applications of PEG and OEG in Medicines and Delivery Formulations

Table 1 Representative Applications of PEG and OEG in Medicines and Delivery Formulations
Tap to enlarge

Application Category

Brand and Generic Name

Company

PEG Structure or Linkage

Main Application

Year of First FDA Approval

Protein and peptide modification

Yuviwel — navepegritide

Ascendis

Two sets of branched 20 kDa mPEG; releasable CNP prodrug

Achondroplasia

2026; accelerated approval

Loargys — pegzilarginase-nbln

Immedica

Arginase modified at multiple sites with 5 kDa mPEG

Arginase 1 deficiency

2026

Yipeisheng — PEGylated growth hormone

Xiamen Amoytop Biotech

Growth hormone modified with one 40 kDa Y-shaped branched PEG

Growth failure due to growth hormone deficiency in children aged 3 years and older

2025; China NMPA

Yorvipath — palopegteriparatide

Ascendis

Approximately 40 kDa PEG carrier; releasable PTH prodrug

Hypoparathyroidism

2024

Zilbrysq — zilucoplan

UCB

Defined-length PEG24 connecting the cyclic peptide to its lipid side chain

Generalized myasthenia gravis

2023

Elfabrio — pegunigalsidase alfa-iwxj

Chiesi / Protalix

An average of approximately nine 2.3 kDa PEG chains crosslink the enzyme dimer

Fabry disease

2023

Syfovre — pegcetacoplan

Apellis

Approximately 40 kDa linear PEG connects two cyclic peptides

Geographic atrophy secondary to age-related macular degeneration

2023

Rolvedon — eflapegrastim-xnst

Spectrum / Hanmi

3.4 kDa PEG links a G-CSF analogue to Fc

Reduction in the risk of chemotherapy-related febrile neutropenia

2022

Besremi — ropeginterferon alfa-2b-njft

PharmaEssentia

Interferon modified with approximately 40 kDa branched PEG

Polycythemia vera

2021

Skytrofa — lonapegsomatropin-tcgd

Ascendis

Approximately 40 kDa branched PEG; releasable growth hormone prodrug

Growth hormone deficiency

2021

Empaveli — pegcetacoplan

Apellis

Approximately 40 kDa linear PEG connects two cyclic peptides

Paroxysmal nocturnal hemoglobinuria and other indications

2021

Esperoct — turoctocog alfa pegol

Novo Nordisk

Site-specific glycoPEGylation of factor VIII with 40 kDa PEG

Hemophilia A

2019

Fulaimei — polyethylene glycol loxenatide

Jiangsu Hansoh Pharmaceutical

Approximately 40 kDa branched PEG covalently linked to the thiol of loxenatide through a maleimide group

Glycemic control in adults with type 2 diabetes

2019; China NMPA

Palynziq — pegvaliase-pqpz

BioMarin

Phenylalanine ammonia lyase modified at multiple sites with individual 20 kDa PEG chains

Phenylketonuria

2018

Revcovi — elapegademase-lvlr

Leadiant

Recombinant adenosine deaminase covalently modified with mPEG

Severe combined immunodeficiency associated with ADA deficiency

2018

Asparlas — calaspargase pegol-mknl

Servier

Asparaginase modified with approximately 31–39 chains of 5 kDa SC-PEG

Acute lymphoblastic leukemia

2018

Jivi — damoctocog alfa pegol

Bayer

Factor VIII modified with 60 kDa branched PEG

Hemophilia A

2018

Rebinyn — nonacog beta pegol

Novo Nordisk

Site-specific glycoPEGylation of factor IX with 40 kDa PEG

Hemophilia B

2017

Pegberon — peginterferon alfa-2b

Xiamen Amoytop Biotech

Recombinant human interferon alfa-2b covalently modified with 40 kDa Y-shaped branched PEG

Chronic hepatitis B and chronic hepatitis C in adults

2016; China, former CFDA

Adynovate — rurioctocog alfa pegol

Baxalta / Takeda

Factor VIII modified with individual 20 kDa PEG chains

Hemophilia A

2015

Plegridy — peginterferon beta-1a

Biogen

Interferon modified with 20 kDa linear mPEG

Relapsing multiple sclerosis

2014

Omontys — peginesatide

Affymax / Takeda

Erythropoietin-mimetic peptide modified with approximately 40 kDa branched PEG

Anemia associated with chronic kidney disease

2012; approval withdrawn

Sylatron — peginterferon alfa-2b

Merck

Interferon modified with 12 kDa mPEG

Adjuvant treatment of melanoma

2011; discontinued

Krystexxa — pegloticase

Savient

Uricase modified at multiple sites with individual 10 kDa mPEG chains

Chronic gout refractory to conventional treatment

2010

Cimzia — certolizumab pegol

UCB

Anti-TNFα Fab′ modified with approximately 40 kDa branched PEG

Inflammatory diseases including rheumatoid arthritis

2008

Mircera — methoxy PEG-epoetin beta

Roche

Erythropoietin modified with approximately 30 kDa linear mPEG

Anemia associated with chronic kidney disease

2007

Somavert — pegvisomant

Pfizer

Growth hormone receptor antagonist modified with individual 5 kDa PEG chains

Acromegaly

2003

Neulasta — pegfilgrastim

Amgen

G-CSF modified with 20 kDa linear mPEG

Reduction in the risk of chemotherapy-related febrile neutropenia and other indications

2002

Pegasys — peginterferon alfa-2a

Roche

Interferon modified with approximately 40 kDa branched PEG

Chronic hepatitis B and C

2002

Pegintron — peginterferon alfa-2b

Schering / Merck

Interferon modified with 12 kDa mPEG

Chronic hepatitis C

2001; discontinued

Oncaspar — pegaspargase

Enzon

Asparaginase modified at multiple sites with individual 5 kDa mPEG chains

Acute lymphoblastic leukemia

1994

Adagen — pegademase bovine

Enzon

Bovine adenosine deaminase modified with approximately 11–17 chains of 5 kDa mPEG

Severe combined immunodeficiency associated with ADA deficiency

1990; discontinued

PEGylated growth factors

Ennumo — pegfilgrastim-pccg

Accord BioPharma

Approximately 20 kDa PEG covalently attached to G-CSF

Prevention of post-chemotherapy neutropenia and related infection risk

2026

Armlupeg — pegfilgrastim-unne

Lupin

Approximately 20 kDa PEG covalently attached to G-CSF

2025

Stimufend — pegfilgrastim-fpgk

Fresenius Kabi

Approximately 20 kDa PEG covalently attached to G-CSF

2022

Fylnetra — pegfilgrastim-pbbk

Amneal

Approximately 20 kDa PEG covalently attached to G-CSF

2022

Nyvepria — pegfilgrastim-apgf

Pfizer

Approximately 20 kDa PEG covalently attached to G-CSF

2020

Ziextenzo — pegfilgrastim-bmez

Sandoz

Approximately 20 kDa PEG covalently attached to G-CSF

2019

Udenyca — pegfilgrastim-cbqv

Coherus

Approximately 20 kDa PEG covalently attached to G-CSF

2018

Fulphila — pegfilgrastim-jmdb

Mylan / Biocon

Approximately 20 kDa PEG covalently attached to G-CSF

2018

Nucleic acid aptamers

Izervay — avacincaptad pegol

Iveric Bio / Astellas

Approximately 43 kDa branched PEG attached to an RNA aptamer

Geographic atrophy

2023

Macugen — pegaptanib sodium

Eyetech / Pfizer

Approximately 40 kDa PEG attached to an RNA aptamer

Wet age-related macular degeneration

2004; discontinued

Small molecules and short OEG

Movantik — naloxegol

AstraZeneca / Nektar

Defined-length PEG7 side chain

Opioid-induced constipation

2014

Asclera — polidocanol

Kreussler

C12 alkyl group with a polyoxyethylene chain averaging approximately 9 repeat units; average molecular weight of the whole molecule approximately 600 Da

Sclerotherapy of spider and reticular veins of the lower limbs

2010

Varithena — polidocanol injectable foam

Biocompatibles

Same polyoxyethylene structure as polidocanol; foam formulation

Certain varicose veins of the lower limbs

2013

Lipidated peptide drugs with short OEG spacers

Ozempic / Rybelsus / Wegovy — semaglutide

Novo Nordisk

Two AEEA-type OEG spacer units between the peptide and a C18 fatty diacid

Type 2 diabetes or weight management, depending on the brand

2017 / 2019 / 2021

Mounjaro / Zepbound — tirzepatide

Eli Lilly

Two AEEA-type OEG spacer units connected to a C20 fatty diacid side chain

Type 2 diabetes or weight management, depending on the brand

2022 / 2023

Awiqli — insulin icodec-abae

Novo Nordisk

Lipid side chain containing two AEEA-type OEG spacer units

Type 2 diabetes in adults

2026

ADCs with PEG linkers

Trodelvy — sacituzumab govitecan-hziy

Immunomedics / Gilead

CL2A linker containing PEG8; SN-38 payload

Certain breast cancers

2020

Zynlonta — loncastuximab tesirine-lpyl

ADC Therapeutics

Tesirine linker containing PEG8; PBD dimer payload

Relapsed or refractory large B-cell lymphoma

2021

Sustained-release delivery carriers

Dextenza — dexamethasone insert

Ocular Therapeutix

PEG-based hydrogel containing dexamethasone

Postoperative ocular inflammation and pain and other indications

2018

Uzedy — risperidone

Teva / MedinCell

Copolymer containing PEG and polylactide segments for a long-acting injectable formulation

Schizophrenia and other indications

2023

Sustol — granisetron

Heron

Poly(ortho ester) carrier containing triethylene glycol, together with mPEG550

Prevention of chemotherapy-related nausea and vomiting

2016; discontinued

PEG-modified nanoparticles and LNPs

Doxil — liposomal doxorubicin

Sequus

MPEG2000-DSPE; PEGylated liposome

Ovarian cancer, Kaposi’s sarcoma, multiple myeloma, and other indications

1995

Onivyde — liposomal irinotecan

Merrimack

MPEG2000-DSPE; PEGylated liposome

Pancreatic adenocarcinoma

2015

Onpattro — patisiran

Alnylam

PEG2000-C-DMG; siRNA-LNP

Polyneuropathy associated with hereditary transthyretin amyloidosis

2018

Comirnaty — COVID-19 mRNA vaccine

BioNTech / Pfizer

ALC-0159, a lipid containing approximately 2 kDa PEG

Prevention of COVID-19

2021

Spikevax — COVID-19 mRNA vaccine

Moderna

PEG2000-DMG; mRNA-LNP

Prevention of COVID-19

2022

mResvia — RSV vaccine

Moderna

PEG2000-DMG; mRNA-LNP

Prevention of RSV-associated lower respiratory tract disease

2024

mNexspike — COVID-19 mRNA vaccine

Moderna

PEG2000-DMG; mRNA-LNP

Prevention of COVID-19

2025

mFlusiva — influenza mRNA vaccine

Moderna

PEG2000-DMG; mRNA-LNP

Prevention of influenza in people aged 50 years and older

2026

COVID-19 Vaccine mRNA

Yuxi Walvax, a subsidiary of Walvax Biotechnology

DMG-PEG2000; mRNA-LNP; average PEG segment molecular weight approximately 2 kDa

Prevention of COVID-19 in people aged 18 years and older

2026; China NMPA

Intismeran autogene (V940 / mRNA-4157)

Merck / Moderna

PEG-DMG; mRNA-LNP

Personalized cancer immunotherapy under investigation as adjuvant treatment after melanoma surgery

Not yet approved; Phase 3 success

Note: Unless otherwise specified, approval years refer to the first full approval by the US FDA. Entries marked "China" give the year of first approval in China. V940 is an investigational program.

In addition to drug modification and delivery carrier construction, PEG can be used as a pharmaceutical excipient, an active ingredient with a direct therapeutic effect, and a medical material. Representative applications are listed below.

Table 2 Representative Uses of PEG as a Formulation Excipient Active Ingredient and Medical Material

Table 2 Representative Uses of PEG as a Formulation Excipient Active Ingredient and Medical Material
Tap to enlarge

Application Category

Product

PEG Type

Main Role or Use

FDA Approval Date

Formulation excipients

Gris-PEG — griseofulvin

PEG 400 and PEG 8000

Oral formulation of ultramicrosize griseofulvin; PEG serves as a formulation excipient

1975

Targretin — bexarotene capsules

PEG 400

Component of the soft capsule fill in oral bexarotene formulations

1999

Busulfex — busulfan injection

PEG 400

Forms the solvent system for busulfan injection together with other solvents

1999

Walvax COVID-19 mRNA vaccine

DMG-PEG2000

Used in the LNP delivery system of Yuxi Walvax’s COVID-19 mRNA vaccine

2026; China CDE associated review, status A

Active ingredients

MiraLax

PEG 3350

Osmotic laxative; PEG itself is the active ingredient

1999

GoLYTELY

PEG 3350 and electrolytes

Bowel cleansing before colon examination; distinct from use as an ordinary formulation excipient

1984

Excipients for contrast agents

Lumason — sulfur hexafluoride microspheres

PEG 4000

Sulfur hexafluoride microbubble ultrasound contrast agent; PEG is a free excipient in the formulation

2014

Definity — perflutren lipid microspheres

MPEG5000-DPPE

Perflutren microbubble ultrasound contrast agent; the PEG lipid forms part of the microbubble shell

2001

Hydrogel sealants

CoSeal Surgical Sealant

Two reactive PEG derivatives that crosslink upon mixing to form a hydrogel

Adjunctive hemostasis and mechanical sealing in vascular reconstruction

2001

DuraSeal Dural Sealant System

PEG ester crosslinked with trilysine to form a hydrogel

Adjunctive watertight dural closure after suturing in cranial surgery

2005

Precision Polymer Products and Custom Synthesis

From defined-length molecular linkers to the surface materials of complex formulations, drug development is moving beyond selecting a nominal PEG molecular weight toward the joint design of chain length, end groups, topology, and linkages. Precision Polymer offers a range of PEG products and custom synthesis services to support research on drug modification, ADC linkers, nucleic acid delivery, and sustained-release systems.

The following are Precision Polymer’s product categories and selected representative products:

Monofunctional Precision PEG

Methoxy-PEG-Hydroxyl

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Methoxy-PEG-Amine

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Methoxy-PEG-Carboxyl

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Methoxy-PEG-NHS Ester

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Methoxy-PEG-Maleimide

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Cyclic PEG with a PEG Arm and Terminal Hydroxyl

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96

Bifunctional Precision PEG

Hydroxyl-PEG-Hydroxyl

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Amine-PEG-Amine

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Thiol-PEG-Thiol

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Amine-PEG-Carboxyl

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Maleimide-PEG-NHS Ester

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Fmoc-Protected Amine-PEG-Carboxyl

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Tosylate-PEG-Tosylate

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Multifunctional Precision PEG

Y-Shaped Two-Arm Methoxy-PEG-NHS Ester

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Y-Shaped Two-Arm Methoxy-PEG-Maleimide

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Four-Arm PEG-Hydroxyl

Available n values: n=4 · n=8 · n=12 · n=24 · n=45 · n=96

Four-Arm PEG-NHS Ester

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Four-Arm PEG-Thiol

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Eight-Arm PEG-Maleimide

Available n values: n=4 · n=8 · n=12 · n=24 · n=45 · n=96

Precision PEG ADC Linkers

Maleimide-PEG-Val-Cit-PAB-OH

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Maleimide-PEG-Val-Ala-PAB-PNP

Available n values: n=4 · n=8 · n=12 · n=16 · n=24 · n=32

Maleimide-PEG-Gly-Gly-Phe-Gly-Carboxyl

Available n values: n=4 · n=8 · n=12 · n=16 · n=24 · n=32

Maleimide-PEG-Disulfide-Carboxyl

Available n values: n=4 · n=8 · n=12 · n=16 · n=24 · n=32

Amine-PEG-Val-Cit-PAB-OH

Available n values: n=4 · n=8 · n=12 · n=16 · n=24 · n=32

DBCO-PEG-Val-Cit-PAB-OH

Available n values: n=4 · n=8 · n=12 · n=16 · n=24 · n=32

Precision PEG Lipids and Excipients

Methoxy-PEG-DSPE

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Methoxy-PEG-DMG

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Methoxy-PEG-DMA

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Methoxy-PEG-DPPE

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Methoxy-PEG-Cholesterol

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Maleimide-PEG-DSPE

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Cyclic PEG with a PEG Arm and Terminal DSPE

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Polysorbate 80

View product

Precision PEG Block Copolymers

Methoxy-PEG-block-poly(D,L-lactide)

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Methoxy-PEG-block-polycaprolactone

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Methoxy-PEG-block-poly(lactic-co-glycolic acid)

Available n values: n=4 · n=8 · n=12 · n=24 · n=45 · n=96

Methoxy-PEG-block-poly(trimethylene carbonate)

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Methoxy-PEG-block-polysarcosine

Available n values: n=4 · n=8 · n=12 · n=24 · n=45 · n=96

Other Precision Polymers

Precision Polyglycerol

Available n values: n=8 · n=16 · n=24 · n=32

Precision Poly(D,L-lactide)

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Precision Polysarcosine

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

DSPE-poly(oligo(ethylene glycol) methyl ether methacrylate)

Available n values: n=8 · n=16 · n=21 · n=32 · n=45 · n=64

Fluorescent Dyes

Fluorescein-PEG-NHS Ester

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Cy3-PEG-NHS Ester

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Cy5-PEG-Maleimide

Available n values: n=4 · n=8 · n=12 · n=24 · n=45 · n=96

Cy7-PEG-NHS Ester

Available n values: n=8 · n=16 · n=24 · n=32 · n=45 · n=64

Click Chemistry Reagents

Amine-PEG-Azide

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

Alkyne-PEG-Hydroxyl

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

DBCO-PEG-NHS Ester

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

TCO-PEG-NHS Ester

Available n values: n=4 · n=6 · n=8 · n=12 · n=16 · n=24 · n=32 · n=45 · n=64 · n=96 · n=112 · n=192

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