Ruxolitinib Phosphate Powder CAS 1092939-17-7

Ruxolitinib phosphate powder (INCB018424, inc424) is the phosphate form of ruxolitinib. Ruxolitinib is the first clinical, effective and selective Jak1 / 2 inhibitor. In the cell-free test, the IC50 is 3.3nm/2.8nm, and the selectivity of JAK1,JAK2 is more than 130 times higher than that of JAK3. Ruxolitinib kills tumor cells through toxic mitochondrial autophagy. Ruxolitinib can induce autophagy and enhance apoptosis.

How do determine the dose of Lucotinib phosphate for the first time?

Ruxolitinib phosphate powder is known as a targeted drug. It is mainly to inhibit the activation of the whole JAK-STAT channel and reduce the abnormally enhanced signal of this channel, so as to obtain the curative effect. However, it is not only limited to the treatment of a single disease but also can play a role in the treatment of Jak1 locus abnormalities. For example, BCR / ABL classic MPN, jak12 exon mutation, call, APL, and even triple-negative MPN patients. How to determine the dose is mainly related to the patient's hemogram index. For example, for those with platelets greater than 200, the initial dose of INCB018424 is 20mg twice a day. For platelets at 100 ~ 200, the initial dose is 15mg twice a day. For patients with platelet values ranging from 50 to 100, the maximum initial dose of Ruxolitinib is 5 mg twice a day. (this drug may aggravate bone marrow suppression, so the initial oral dose of the patient should be carefully formulated)

How effective is Jakafi in the treatment of vitiligo?

On May 17, 2021, Incyte announced that its topical JAK inhibitor Ruxolitinib cream had reached the primary endpoint and key secondary endpoint in two key phases 3 clinical trials, which significantly improved the skin symptoms of patients with vitiligo on the face and whole body. Ruxolitinib phosphate powder is a topical Jak1 / JAK2 preparation, which has passed the review of the FDA and is used to treat atopic dermatitis in adolescents and adults (aged ≥ 12 years). Earlier, at the 24th World Society of Dermatology (WCD) held in Milan, Italy, in June 2019, Incyte announced the research results of the phase II clinical trial of Ruxolitinib phosphate cream for a small number of patients with vitiligo, that is, the patients with facial leukoplakia area score index of 50 after 24 weeks of treatment were significantly more than those in the control group. The main side effect of the drug is to increase acne by 10% ~ 15%, while other side effects are not obvious. All doses of Ruxolitinib phosphate cream are well tolerated.

Does this product need to be taken for life?

Does Ruxolitinib need to be taken for life? Rusotinib should be taken continuously until the disease progresses or intolerable side effects occur. On this issue, Novartis, a pharmaceutical company, released positive data on the key phase III response study of the anti-cancer drug INCB018424. It was carried out at 109 sites around the world. In the trial, 222 patients with polycythemia vera (PV) who were resistant or intolerant to hydroxyurea were randomized to receive ruxolitinib (10mg, twice a day) or the best treatment (i.e. monotherapy selected by the researchers or observation only). Throughout the study, the dose will be adjusted as needed. The primary endpoints were the proportion of patients whose hematocrit was controlled without bleeding, and a 35% or more reduction in spleen volume from baseline at 32 weeks (as assessed by imaging). In addition to blood safety, the secondary endpoints include complete remission and complete remission.

The results showed that the study reached the primary endpoint of maintaining hematocrit (red blood cell volume) under control without bleeding (a procedure to remove some blood from the body to reduce red blood cell concentration) while reducing the size of the spleen in patients with hydroxyurea resistant or intolerant polycythemia vera. 70% of patients in the Ruxolitinib group achieved hematocrit control or spleen volume reduction, compared with 20% in the best supportive therapy group. The safety of inc424 in the study is consistent with previous studies. Before using inc424, it is necessary to monitor the platelet count. Take different doses of inc424 based on the platelet count. When taking ruxolitinib, patients should detect the whole blood cell count every 2-4 weeks and adjust the dose according to the recovery of the spleen. In the case of data reply, you can stop using this product slowly.

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