NAV

Rurioctocog alfa pegol

Identification

Summary

Rurioctocog alfa pegol is a pegylated recombinant human coagulation factor VIII used to treat and prevent bleeding episodes in patients 12 years and above with hemophilia A.

Generic Name
Rurioctocog alfa pegol
DrugBank Accession Number
DB16007
Background

Rurioctocog alfa pegol is a pegylated recombinant human coagulation factor VIII or antihemophilic factor. Factor VIII is an essential protein involved in normal blood clotting; thus, a deficient level of functional factor VIII is associated with an elevated risk for excessive bleeding caused by spontaneous or secondary events like trauma or surgery.3 Hemophilia A is the most common inherited bleeding disorder leading to deficiency of factor VIII, which is caused by defects in the F8C gene that encodes coagulation factor VIII. Bleeding in joints is a common manifestation of hemophilia A, and bleeding episodes can be severe and life-threatening like intracranial hemorrhage.2 Rurioctocog alfa pegol aims to restore functional levels of factor VIII in patients with hemophilia A to manage and prevent bleeding episodes. It was first approved by the European Commission in January 2018.5

Rurioctocog alfa pegol is a covalent conjugate of octocog alfa, which is a recombinant factor VIII produced by recombinant DNA technology from a Chinese hamster ovary cell line. The presence of the polyethylene glycol (PEG) moiety increases the plasma half-life of the drug, thereby increasing the drug's duration of action.4

Type
Biotech
Groups
Approved, Experimental
Biologic Classification
Protein Based Therapies
Blood factors
Protein Chemical Formula
C12257H17863N3220O3552S83
Protein Average Weight
269812.0 Da (approximate)
Sequences
>Rurioctocog alfa pegol heavy chain
ATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFN
IAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQ
REKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSLYSHVDLVKDLNSGLIGALLVCR
EGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNR
SLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLL
MDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRF
DDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIG
RKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGI
TDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNME
RDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAG
VQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKH
KMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYE
DSYEDISAYLLSKNNAIEPRSFSQNSRHPSTRQKQFNATTIPENDIEKTDPWFAHRTPMP
KIQNVSSSDLLMLLRQSPTPHGLSLSDLQEAKYETFSDDPSPGAIDSNNSLSEMTHFRPQ
LHHSGDMVFTPESGLQLRLNEKLGTTAATELKKLDFKVSSTSNNLISTIPSDNLAAGTDN
TSSLGPPSMPVHYDSQLDTTLFGKKSSPLTESGGPLSLSEENNDSKLLESGLMNSQESSW
GKNVSSTESGRLFKGKRAHGPALLTKDNALFKVSISLLKTNKTSNNSATNRKTHIDGPSL
LIENSPSVWQNILESDTEFKKVTPLIHDRMLMDKNATALRLNHMSNKTTSSKNMEMVQQK
KEGPIPPDAQNPDMSFFKMLFLPESARWIQRTHGKNSLNSGQGPSPKQLVSLGPEKSVEG
QNFLSEKNKVVVGKGEFTKDVGLKEMVFPSSRNLFLTNLDNLHENNTHNQEKKIQEEIEK
KETLIQENVVLPQIHTVTGTKNFMKNLFLLSTRQNVEGSYDGAYAPVLQDFRSLNDSTNR
TKKHTAHFSKKGEEENLEGLGNQTKQIVEKYACTTRISPNTSQQNFVTQRSKRALKQFRL
PLEETELEKRIIVDDTSTQWSKNMKHLTPSTLTQIDYNEKEKGAITQSPLSDCLTRSHSI
PQANRSPLPIAKVSSFPSIRPIYLTRVLFQDNSSHLPAASYRKKDSGVQESSHFLQGAKK
NNLSLAILTLEMTGDQREVGSLGTSATNSVTYKKVENTVLPKPDLPKTSGKVELLPKVHI
YQKDLFPTETSNGSPGHLDLVEGSLLQGTEGAIKWNEANRPGKVPFLRVATESSAKTPSK
LLDPLAWDNHYGTQIPKEEWKSQEKSPEKTAFKKKDTILSLNACESNHAIAAINEGQNKP
EIEVTWAKQGRTERLCSQNPPVLKRHQR
>Rurioctocog alfa pegol light chain
EITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWD
YGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVE
DNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKD
EFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKS
WYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMG
SNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHA
GMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPF
SWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFG
NVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDA
QITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGV
KSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRI
HPQSWVHQIALRMEVLGCEAQDLY
References:
  1. KEGG Drug: Rurioctocog alfa pegol [Link]
Download FASTA Format
Synonyms
  • BAX 855
  • Rurioctocog alfa pegol
  • SHP660
  • TAK-660
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Pharmacology

Indication

Rurioctocog alfa pegol is indicated for the treatment and prophylaxis of bleeding in patients 12 years and above with hemophilia A (congenital factor VIII deficiency).4

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Prophylaxis ofBleeding caused by hemophilia a••••••••••••••••••••••• ••••••••••••••
Management ofBleeding caused by hemophilia a••••••••••••••••••••••• ••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Rurioctocog alfa pegol is a recombinant coagulation factor that promotes blood clotting. In clinical trials, personalized administration of rurioctocog alfa pegol based on each patient's clinical profile led to increased plasma levels of factor VIII and reduced bleeding episodes at six and 12 months of treatment.1 Rurioctocog alfa pegol has a long duration of action compared to octocog alfa: it has an extended half-life of 1.4 to 1.5-fold compared to octocog alfa in adolescents and adults.4

Mechanism of action

Factor VIII plays an essential role in the intrinsic pathway of the blood coagulation cascade: as a cofactor for activated factor IX (FIXa), factor VIII significantly facilitates the conversion of FIXa-mediated transformation of inactive factor X (FX) to its active form (FXa). FXa then promotes the conversion of prothrombin into thrombin, a key serine protease of the coagulation cascade. Proper blood clotting cannot be achieved with the deficient levels of factor VIII, leading to increased excessive bleeding spontaneously or as a result of accidental or surgical trauma.3,4 Hemophilia A is an X-chromosomal linked hereditary disorder of blood coagulation due to defects in the F8C gene that encodes coagulation factor VIII, leading to decreased production of functional factor VIII.2

Rurioctocog alfa pegol is a pegylated recombinant human factor VIII that aims to restore the plasma levels and hemostatic activity of functional factor VIII. It can be used for both prophylactic or on-demand treatment of bleeding episodes associated with hemophilia A.4

TargetActionsOrganism
Avon Willebrand factor
binder
Humans
UCoagulation factor VIII
regulator
Humans
Absorption

Following intravenous administration of rurioctocog alfa pegol, the mean ± SD Cmax was 117 ± 28 IU/dL in adolescents and 145 ± 29 IU/dL in adults.4

Volume of distribution

Following intravenous administration, the mean ± SD volume of distribution at steady-state was 0.54 ± 0.22 dL/kg in adolescents and 0.40 ± 0.09 dL/kg in adults.4

Protein binding

Once rurioctocog alfa pegol enters the circulation, it binds to von Willebrand factor, just like how an endogenous factor VIII would. There is limited information on the binding profile of rurioctocog alfa pegol to plasma proteins other than von Willebrand factor.4

Metabolism

There is limited information regarding the metabolism of rurioctocog alfa pegol; however, it is expected to undergo catabolism just like endogenous coagulation factor VIII. Metabolism pathways and CYP involvement are not known to exist regarding coagulation factors.6

Route of elimination

There is limited information regarding the route of elimination of rurioctocog alfa pegol.

Half-life

Following intravenous administration of rurioctocog alfa pegol, the mean ± SD terminal half-life was 13.80 ± 4.01 hours in adolescents and 15.01 ± 3.89 hours in adults.4

Clearance

Following intravenous administration of rurioctocog alfa pegol, the mean ± SD clearance was 2.58 ± 0.84 mL/(kg·h) in adolescents and 2.16 ± 0.75 mL/(kg·h) in adults.4

Adverse Effects
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Toxicity

There is no information on the LD50 of rurioctocog alfa pegol. No symptoms of overdose with recombinant coagulation factor VIII have been reported.4

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
Integrate drug-drug
interactions in your software
AbciximabThe therapeutic efficacy of Rurioctocog alfa pegol can be decreased when used in combination with Abciximab.
AcenocoumarolThe therapeutic efficacy of Rurioctocog alfa pegol can be decreased when used in combination with Acenocoumarol.
Alpha-1-proteinase inhibitorAlpha-1-proteinase inhibitor may increase the thrombogenic activities of Rurioctocog alfa pegol.
AlteplaseThe therapeutic efficacy of Rurioctocog alfa pegol can be decreased when used in combination with Alteplase.
Aminocaproic acidThe risk or severity of adverse effects can be increased when Aminocaproic acid is combined with Rurioctocog alfa pegol.
Food Interactions
No interactions found.

Products

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International/Other Brands
Adynovi (Baxalta)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AdynoviInjection, powder, for solution500 IUIntravenousBaxalta Innovations Gmb H2020-12-16Not applicableEU flag
AdynoviInjection, powder, for solution1000 IUIntravenousBaxalta Innovations Gmb H2020-12-16Not applicableEU flag
AdynoviInjection, powder, for solution250 IUIntravenousBaxalta Innovations Gmb H2020-12-16Not applicableEU flag
AdynoviInjection, powder, for solution1000 IUIntravenousBaxalta Innovations Gmb H2020-12-16Not applicableEU flag
AdynoviInjection, powder, for solution2000 IUIntravenousBaxalta Innovations Gmb H2020-12-16Not applicableEU flag

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
Not Available
CAS number
1417412-83-9

References

General References
  1. Klamroth R, Windyga J, Radulescu V, Collins PW, Stasyshyn O, Ibrahim HM, Engl W, Tangada SD, Savage W, Ewenstein B: Rurioctocog alfa pegol PK-guided prophylaxis in hemophilia A: results from the phase 3 PROPEL study. Blood. 2021 Apr 1;137(13):1818-1827. doi: 10.1182/blood.2020005673. [Article]
  2. Castaldo G, D'Argenio V, Nardiello P, Zarrilli F, Sanna V, Rocino A, Coppola A, Di Minno G, Salvatore F: Haemophilia A: molecular insights. Clin Chem Lab Med. 2007;45(4):450-61. doi: 10.1515/CCLM.2007.093. [Article]
  3. Klinge J, Ananyeva NM, Hauser CA, Saenko EL: Hemophilia A--from basic science to clinical practice. Semin Thromb Hemost. 2002 Jun;28(3):309-22. doi: 10.1055/s-2002-32667. [Article]
  4. Summary of Product Characteristics: ADYNOVI (rurioctocog alfa pegol) intravenous injection [Link]
  5. European Medicines Agency Medicines: Adynovi (rurioctocog alfa pegol) [Link]
  6. European Medicines Agency Assessment Report: ADYNOVI, INN (rurioctocog alfa pegol) [Link]
Wikipedia
Factor_VIII_(medication)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19) / Hemophilia A1
3Active Not RecruitingTreatmentHemophilia A1
3CompletedPreventionHemophilia A2
3CompletedTreatmentHemophilia A2
2, 3CompletedPreventionHemophilia A1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
SolutionIntravenous250 UI
Powder1000 IU
Powder1500 IU
Powder2000 IU
Powder250 IU
Powder3000 IU
Powder500 IU
Powder750 IU
Injection, powder, for solutionIntravenous1000 IU
Injection, powder, for solutionIntravenous2000 IU
Injection, powder, for solutionIntravenous250 IU
Injection, powder, for solutionIntravenous3000 IU
Injection, powder, for solutionIntravenous500 IU
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available

Targets

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Details1. von Willebrand factor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
General Function
Protein n-terminus binding
Specific Function
Important in the maintenance of hemostasis, it promotes adhesion of platelets to the sites of vascular injury by forming a molecular bridge between sub-endothelial collagen matrix and platelet-surf...
Gene Name
VWF
Uniprot ID
P04275
Uniprot Name
von Willebrand factor
Molecular Weight
309261.83 Da
References
  1. Summary of Product Characteristics: ADYNOVI (rurioctocog alfa pegol) intravenous injection [Link]
Details2. Coagulation factor VIII
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Regulator
General Function
Oxidoreductase activity
Specific Function
Factor VIII, along with calcium and phospholipid, acts as a cofactor for factor IXa when it converts factor X to the activated form, factor Xa.
Gene Name
F8
Uniprot ID
P00451
Uniprot Name
Coagulation factor VIII
Molecular Weight
267007.42 Da
References
  1. Klamroth R, Windyga J, Radulescu V, Collins PW, Stasyshyn O, Ibrahim HM, Engl W, Tangada SD, Savage W, Ewenstein B: Rurioctocog alfa pegol PK-guided prophylaxis in hemophilia A: results from the phase 3 PROPEL study. Blood. 2021 Apr 1;137(13):1818-1827. doi: 10.1182/blood.2020005673. [Article]

Drug created at December 10, 2020 21:45 / Updated at February 10, 2022 08:54