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| Primary information |
|---|
| ID | 16382 |
| Therapeutic ID | Th1892 |
| Protein Name | Rurioctocog alfa pegol |
| Sequence | >Th1892_Rurioctocog_alfa_pegol
ATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSLYSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNSRHPSTRQKQFNATTIPENDIEKTDPWFAHRTPMPKIQNVSSSDLLMLLRQSPTPHGLSLSDLQEAKYETFSDDPSPGAIDSNNSLSEMTHFRPQLHHSGDMVFTPESGLQLRLNEKLGTTAATELKKLDFKVSSTSNNLISTIPSDNLAAGTDNTSSLGPPSMPVHYDSQLDTTLFGKKSSPLTESGGPLSLSEENNDSKLLESGLMNSQESSWGKNVSSTESGRLFKGKRAHGPALLTKDNALFKVSISLLKTNKTSNNSATNRKTHIDGPSLLIENSPSVWQNILESDTEFKKVTPLIHDRMLMDKNATALRLNHMSNKTTSSKNMEMVQQKKEGPIPPDAQNPDMSFFKMLFLPESARWIQRTHGKNSLNSGQGPSPKQLVSLGPEKSVEGQNFLSEKNKVVVGKGEFTKDVGLKEMVFPSSRNLFLTNLDNLHENNTHNQEKKIQEEIEKKETLIQENVVLPQIHTVTGTKNFMKNLFLLSTRQNVEGSYDGAYAPVLQDFRSLNDSTNRTKKHTAHFSKKGEEENLEGLGNQTKQIVEKYACTTRISPNTSQQNFVTQRSKRALKQFRLPLEETELEKRIIVDDTSTQWSKNMKHLTPSTLTQIDYNEKEKGAITQSPLSDCLTRSHSIPQANRSPLPIAKVSSFPSIRPIYLTRVLFQDNSSHLPAASYRKKDSGVQESSHFLQGAKKNNLSLAILTLEMTGDQREVGSLGTSATNSVTYKKVENTVLPKPDLPKTSGKVELLPKVHIYQKDLFPTETSNGSPGHLDLVEGSLLQGTEGAIKWNEANRPGKVPFLRVATESSAKTPSKLLDPLAWDNHYGTQIPKEEWKSQEKSPEKTAFKKKDTILSLNACESNHAIAAINEGQNKPEIEVTWAKQGRTERLCSQNPPVLKRHQR
|
| Molecular Weight | 269812.0 Da |
| Chemical Formula | 12257H17863N3220O3552S83 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| 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. |
| Description | NA |
| Indication/Disease | 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). |
| 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. |
| 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. |
| Toxicity | There is no information on the LD50 of rurioctocog alfa pegol. No symptoms of overdose with recombinant coagulation factor VIII have been reported. |
| 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. |
| 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. |
| 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. |
| 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. |
| Categories | Amino Acids, Peptides, and Proteins,Biological Factors,Blood Coagulation Factors,Blood Proteins,Coagulants,Factor VIII,Hematologic Agents,Hemostatics,Pegylated agents,Protein Precursors,Proteins,Recombinant Proteins |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | von Willebrand factor, Coagulation factor VIII |
| Brand Name | Adynovi |
| Company | Baxalta Innovations Gmb H |
| Brand Description | Baxalta Innovations Gmb H |
| Prescribed For | Intravenous |
| Chemical Name | 1000 IU |
| Formulation | NA |
| Physical Appearance | Hypersensitivity (allergic) reactions are uncommon with Adynovi (affecting up to 1 in 100 people) and may include swelling, burning and stinging at the injection site, chills, flushing, itchy rash, headache, hives, low blood pressure, lethargy, nausea and vomiting, restlessness, a rapid heartbeat, tightness of the chest and wheezing. In some cases these reactions can become severe. |
| Route of Administration | Adynovi contains the active substance rurioctocog alfa pegol. |
| Recommended Dosage | Adynovi is a medicine used to treat and prevent bleeding in patients with haemophilia A, an inherited bleeding disorder caused by lack of a clotting protein called factor VIII. It can be used in adults and children from 12 years of age. |
| Contraindication | NA |
| Side Effects | NA |
| Useful Link 1 | Link |
| Useful Link 2 | Link |
| Remarks | NA |