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Primary information
ThPP ID	Th1142
Therapeutic Peptide/Protein Name	Obinutuzumab
Sequence	N.A. view full sequnce in fasta
Functional Classification	IIb
Molecular Weight	146100
Chemical Formula	C6512H10060N1712O2020S44
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	28.4 days
Description	Humanized monoclonal antibody used along with chlorambucil for the treatment of chronic lymphocytic leukemia. It was approved by the FDA in November 2013 and is marketed under the brand name Gazyva. It carries a black box warning of fatal Hepatitis B Virus (HBV) reactivation and fatal Progressive Multifocal Leukoencephalopathy (PML).
Indication/Disease	Obinutuzumab is used as a combination treatment with chlorambucil to treat patients with untreated chronic lymphocytic leukemia.
Pharmacodynamics	Obinutuzumab is more potent than rituximab in depleting B-cells, antitumor activity, and tumor regression.
Mechanism of Action	In contrast to rituximab, which is a classic type I CD20 antibody, obinutuzumab binds to type II CD20 antibodies. This allows obinutuzumab to have a much higher induction of antibody-dependant cytotoxicity and a higher direct cytotoxic effect than the classic CD20 antibodies.
Toxicity	The most serious toxicities observed with obinutuzumab are Hepatitis B virus (HBV) reactivation and progressive multifocal leukoencephalopathy (PML). HBV reactivation can occur with all anti-CD20 antibodies and can result in hepatic failure, fulminant hepatitis, and death. PML occurs as a result of JC virus infection and can be fatal as well. Other common but less serious adverse reactions include infusion reactions (pre-treat with glucocorticoids, acetaminophen, and anti-histamine to prevent this), neutropenia, thrombocytopenia, and Tumor Lysis Syndrome (TLS) (pre-treat patients, especially with a high lymphocyte count and/or a high tumor burden, with anti-hyperuricemics and hydration). It is also recommended to NOT administer live virus vaccinations prior to or during obinutuzumab treatment.
Metabolism	Obinutuzumab is not metabolized by the liver.
Absorption	Obinutuzumab is administered intravenously, so its absorption is 100%.
Volume of Distribution	Obinutuzumab has a volume of distribution of about 3.8 L.
Clearance	The clearance of obinutuzumab is 0.09L/day.
Categories	Antineoplastic Agents
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	N.A.
Target	B-lymphocyte antigen CD20
Information of corresponding available drug in the market
Brand Name	Gazyva
Company	Genentech
Brand Discription	GAZYVA (obinutuzumab) is a humanized anti-CD20 monoclonal antibody of the IgG1 subclass. It recognizes a specific epitope of the CD20 molecule found on B-cells. The molecular mass of the antibody is approximately 150 kDa.
Prescribed for	chronic lymphocytic leukemia (CLL)
Chemical Name	N.A.
Formulation	GAZYVA is supplied at a concentration of 25 mg/mL in 1000 mg single use vials. The product is formulated in 20 mM L-histidine/L-histidine hydrochloride, 240 mM trehalose, 0.02% poloxamer 188. The pH is 6.0.
Physcial Appearnce	GAZYVA is produced by mammalian cell (CHO) suspension culture. GAZYVA is a sterile, clear, colorless to slightly brown, preservative free liquid concentrate for intravenousadministration.
Route of Administration	Intravenous infusion
Recommended Dosage	Each dose of GAZYVA is 1000 mg, administered intravenously, with the exception of the first infusions in cycle 1, which are administered on day 1 (100 mg) and day 2 (900 mg).
Contraindication	N.A.
Side Effects	Hepatitis B reactivation, Progressive multifocal leukoencephalopathy, Infusion reactions, Tumor lysis syndrome, Infections, Neutropenia, Thrombocytopenia.
Useful Link	http://www.rxlist.com/gazyva-drug.htm http://www.gazyva.com/ http://www.roche.com/media/store/releases/med-cor-2013-11-01.htm
PubMed ID	25634683, 25586272, 25538980, 25355689, 25353187
3-D Structure	N.A.