Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6512H10060N1712O2020S44
Phân tử khối
146100 daltons
Dược Lực Học :
Obinutuzumab is more potent than rituximab in depleting B-cells, antitumor activity, and tumor regression.
Cơ Chế Tác Dụng :
Obinutuzumab is a humanized monoclonal antibody used as a combination treatment with chlorambucil to treat patients with untreated chronic lymphocytic leukemia. It was approved by the FDA in November 2013 and is marketed under the brand name Gazyva. There is a black box warning of fatal Hepatitis B Virus (HBV) reactivation and fatal Progressive Multifocal Leukoencephalopathy (PML).
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.
Dược Động Học :
▧ Absorption :
Obinutuzumab is administered intravenously, so its absorption is 100%.
▧ Volume of Distribution :
Obinutuzumab has a volume of distribution of about 3.8 L.
▧ Protein binding :
Obinutuzumab does not bind to plasma proteins.
▧ Metabolism :
Obinutuzumab is not metabolized by the liver.
▧ Route of Elimination :
The route of elimination of obinutuzumab was not indicated (FDA label).
▧ Half Life :
The half life of obinutuzumab is 28.4 days.
▧ Clearance :
The clearance of obinutuzumab is 0.09L/day.
Độc Tính :
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.
Chỉ Định :
Obinutuzumab is used as a combination treatment with chlorambucil to treat patients with untreated chronic lymphocytic leukemia.
Tương Tác Thuốc :
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Aliskiren
Obinutuzumab antihypertensive effect may be enhanced. Administration of antihypertensives should be withheld 12 hours before infusion of obinutuzumab and 1 hour after the end of infusion.
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Belimumab
Avoid combination due to enhanced toxic effects of monoclonal antibody.
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Clozapine
Risk of agranulocytosis may be increased due to enhanced adverse effects of clozapine by myelosuppressive agents. It is recommanded that combination may be avoided.
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Denosumab
Monitor therapy due to increased risk of infections due to adverse effects of immunosuppressants.
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Eptifibatide
Monitor therapy due to increased risk of bleeding events.
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Leflunomide
Consider modifying therapy. Risk of hematologic toxicity of leflunomide may be increased due to enhanced adverse effects.
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Natalizumab
Avoid combination due to enhanced adverse effects of natalizumab.
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Pimecrolimus
Avoid combination due to enhanced immunosuppressive effects.
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Roflumilast
Consider therapy modification due to enhanced immunosuppressive effect.
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Sipuleucel-T
Monitor therapy due to diminished therapeutic effect of sipuleucel-t.
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Tacrolimus
Avoid combination due to enhanced adverse effects of immunosuppressants.
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Tofacitinib
Avoid combination due to enhanced immunosuppressive effect.
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Trastuzumab
Monitor therapy due to enhanced neutropenic effect of immunosuppressants
Liều Lượng & Cách Dùng :
Injection - Intravenous - 1000MG/40ML
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National Drug Code Directory