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    Damoctocog Alfa Pegol

    FINISHED DOSAGE FORMULATIONS

    DIGITAL CONTENT

    GLOBAL SALES INFORMATION

    PharmaCompass
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    2D Structure
    Also known as: Unii-by4tsk952y, Damoctocog alfa pegol [inn], By4tsk952y, 1363853-26-2, Des-(743-1636)-(1804-(s-(1-(3-((3-(2,3-bis(omega-methoxypoly(oxyethylene))propoxy)propyl)amino)-3-oxopropyl)-2,5-dioxopyrrolidin-3-yl)-l-cysteine)(k>c))human coagulation factor viii, Q27274954
    Molecular Formula
    C22H39N3O10S
    Molecular Weight
    537.6  g/mol
    InChI Key
    UGQOPAJHKRJXBG-ADKAHSJRSA-N
    In recent years, various extended half-life factor VIII and factor IX preparations have been studied and gained approval. In order to extend half-lives, techniques such as fusion to protein conjugates (Fc part of IgG1 or albumin), chemical modification (PEGylation), and protein sequence modification have been utilized. Also known as, BAY94-9027, Damoctocog alfa pegol is a longer-acting Factor VIII therapy formulated with polyethylene glycol (PEG) to reduce the number of infusions necessary to prevent bleeds in patients diagnosed with Haemophilia A. This product has been engineered by Bayer and a biological license application has been filed with the FDA in August 2017 and FDA approved in August 2018.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    (2R)-2-amino-3-[1-[3-[3-[2,3-bis(2-methoxyethoxy)propoxy]propylamino]-3-oxopropyl]-2,5-dioxopyrrolidin-3-yl]sulfanylpropanoic acid
    2.1.2 InChI
    InChI=1S/C22H39N3O10S/c1-31-8-10-34-14-16(35-11-9-32-2)13-33-7-3-5-24-19(26)4-6-25-20(27)12-18(21(25)28)36-15-17(23)22(29)30/h16-18H,3-15,23H2,1-2H3,(H,24,26)(H,29,30)/t16?,17-,18?/m0/s1
    2.1.3 InChI Key
    UGQOPAJHKRJXBG-ADKAHSJRSA-N
    2.1.4 Canonical SMILES
    COCCOCC(COCCCNC(=O)CCN1C(=O)CC(C1=O)SCC(C(=O)O)N)OCCOC
    2.1.5 Isomeric SMILES
    COCCOCC(COCCCNC(=O)CCN1C(=O)CC(C1=O)SC[C@@H](C(=O)O)N)OCCOC
    2.2 Synonyms
    2.2.1 Depositor-Supplied Synonyms

    1. Unii-by4tsk952y

    2. Damoctocog Alfa Pegol [inn]

    3. By4tsk952y

    4. 1363853-26-2

    5. Des-(743-1636)-(1804-(s-(1-(3-((3-(2,3-bis(omega-methoxypoly(oxyethylene))propoxy)propyl)amino)-3-oxopropyl)-2,5-dioxopyrrolidin-3-yl)-l-cysteine)(k>c))human Coagulation Factor Viii

    6. Q27274954

    2.3 Create Date
    2014-11-22
    3 Chemical and Physical Properties
    Molecular Weight 537.6 g/mol
    Molecular Formula C22H39N3O10S
    XLogP3-4.7
    Hydrogen Bond Donor Count3
    Hydrogen Bond Acceptor Count12
    Rotatable Bond Count22
    Exact Mass537.23561562 g/mol
    Monoisotopic Mass537.23561562 g/mol
    Topological Polar Surface Area201 Ų
    Heavy Atom Count36
    Formal Charge0
    Complexity685
    Isotope Atom Count0
    Defined Atom Stereocenter Count1
    Undefined Atom Stereocenter Count2
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Indication

    Indicated for use in previously treated adults and adolescents (12 years of age and above) with hemophilia A (congenital Factor VIII deficiency) for: On-demand treatment and control of bleeding episodes, perioperative management of bleeding, and routine prophylaxis to reduce the frequency of bleeding episodes.

    FDA Label

    Treatment and prophylaxis of bleeding in previously treated patients 12 years of age with haemophilia A (congenital factor VIII deficiency).

    Treatment of hereditary factor VIII deficiency

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    This agent is engineered to prolong blood FVIII activity while maintaining coagulation activity using PEGylation, where a PEG (Polyethylene glycol) molecule is continually attached to the factor VIII protein at a specific site,. This prevents and controls bleeding episodes associated with hemophilia A. The aPTT is prolonged in people diagnosed with hemophilia A. The determination of aPTT is a conventional in vitro assay for assessing the biological activity of Factor VIII. Treatment with damoctogog alfa pegol normalizes the aPTT similar to that achieved with plasma-derived Factor VIII. The administration of this agent increases plasma levels of Factor VIII and can temporarily correct the coagulation defect that exists in hemophilia A patients.

    5.2 ATC Code

    B02BD02

    5.3 Absorption, Distribution and Excretion

    Absorption

    After a single dose, AUC (area under the curve) was 1640 550 with a dose of 25 IU/kg.

    Clearance

    142 33 mL/h on with a dose of 25 IU/kg and 121 53 mL/h with a dose of 60 IU/kg.

    5.4 Biological Half-Life

    18.6 4.6h after a single dose

    5.5 Mechanism of Action

    This drug is a site-specifically PEGylated recombinant antihemophilic factor, which temporarily replaces the missing coagulation Factor VIII. The site-specific PEGylation in the A3 domain reduces binding to the physiological Factor VIII clearance receptors resulting in a longer half-life and increased AUC (area under the curve). The active protein, prior to conjugation is a recombinant B-domain deleted human coagulation Factor VIII (BDD-rFVIII) produced by recombinant DNA technology in Baby Hamster Kidney (BHK) cells. Damoctagol alfa pegol is manufactured by site-specific conjugation of the BDD-rFVIII variant K1804C at the cysteine amino acid position 1804 (within the A3 domain) with a single maleimide-derivatized, 60 kilodalton (kDa) branched PEG (two 30 kDa PEG) moiety. The A3 domain was identified and selected for conjugation to provide both a continual coagulation activity and high PEGylation efficiency.