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Lorlatinib is a kinase inhibitor for oral administration used to treat cancer. A kinase inhibitor is an enzyme inhibitor that can block the action of protein kinases.
Lorlatinib is taken orally, in the form of tablets. Lorlatinib may be taken with or without food. The drug should be swallowed whole, without chewing, crushing or breaking the tablet. You should take this medicine at the same time each day. If you miss a dose, take it as soon as you remember unless it is less than 4 hours until the next dose. Do not take 2 doses at the same time to make up for a missed dose.
When using the drug, you need to limit the use of some foods, including: Grapefruit, grapefruit juice, Ketoconazole, Rifampin, Phenytoin, St. John's wort and Fentanyl. Also, tell your treating doctor about all other medicines and supplements you are taking.
What Is The Mechanism Of Lorlatinib
Lorlatinib is a targeted therapy drug commonly used in the treatment of non-small cell lung cancer (NSCLC). It specifically caters to patients whose tumors possess certain genetic alterations in the anaplastic lymphoma kinase (ALK) gene or the c-ros oncogene 1 (ROS1) gene.
At the molecular level, Lorlatinib functions as a tyrosine kinase inhibitor (TKI). Tyrosine kinases are enzymes responsible for the activation of many proteins by signaling cellular pathways through the addition of a phosphate group to tyrosine residues on target proteins.
Lorlatinib binds to the ATP-binding pocket of the aberrant ALK and ROS1 tyrosine kinases, inhibiting their activity. By doing so, it effectively halts the phosphorylation process that is crucial for the activation of the downstream signaling cascades.
The mechanism of Lorlatinib involves the selective inhibition of aberrant ALK and ROS1 tyrosine kinases, resulting in the disruption of critical signaling pathways essential for cancer cell survival and proliferation. Its ability to cross the blood-brain barrier enhances its therapeutic efficacy, particularly in patients with brain metastases.
Types of API
Cabozantinib S-Malate
Cabozantinib S-malate is an effective multi receptor tyrosine kinase inhibitor with IC50 values of 0.035, 1.3, 4.6, 7, and 11.3 nM, respectively, for inhibiting VEGFR2, c-Met, Kit, Axl, and Flt3.
Brigatinib
Brigatinib is a anaplastic lymphoma kinase inhibitor used to treat anaplastic lymphoma enzyme positive metastatic non-small cell lung cancer.
Capmatinib Hydrochloride Hydrate
Capmatinib Hydrochloride Hydrate（INCB28060）is a potent, oral, selective, ATP competitive c-Met kinase inhibitor (IC50=0.13nM).
Crizotinib is a kinase inhibitor that works by targeting and blocking receptors found on cancer cells called nonproducing lymphoma kinase (ALK). Crizotinib is used to treat lung cancer that has spread to other parts of the body.
Crizotinib is taken orally, can be taken with food. The patient should swallow the tablet whole with water, do not break, open, crush or chew the tablet.
Dosage of Crizotinib for adults with lung cancer: 250mg x 2 times/day.
Currently, the dose of Crizotinib for children has not been studied and decided. So consult your doctor before giving Crizotinib to a child.
If you forget to take a dose of Crizotinib, take it as soon as you remember. However, if it is almost time for your next dose of Crizotinib, skip the missed dose and take your next dose exactly as directed by your doctor. Never take a double dose of Crizotinib to make up for a missed dose.
Precautions of Crizotinib
Caution should be exercised in patients with history of liver or kidney disease, vision problems, abnormal heart rhythm, prolonged QT syndrome, electrolyte imbalance, who are taking other medications, any allergy, during pregnancy and breastfeeding.
It may cause dizziness, drowsiness, or blurred vision, do not drive a car or operate machinery while taking this medication.
It may reduce platelet counts; avoid injury or bruising.
Avoid contact with people who have infections that may spread to others.
Rarely patient may develop with fatal inflammation of the lungs (pneumonitis) with the following symptoms: trouble in breathing, shortness of breath, cough, or fever. If it is so consult with your healthcare provider immediately.
What Is The Mechanism Of Crizotinib
Crizotinib is a targeted cancer therapy primarily used for the treatment of non-small cell lung cancer (NSCLC) that harbors specific genetic alterations.
At the core of Crizotinib's mechanism is its inhibition of the anaplastic lymphoma kinase (ALK) protein. ALK is a receptor tyrosine kinase, which means it is involved in the signaling pathways that regulate cell growth and survival.
One of the most common ALK gene rearrangements in involves the fusion of the ALK gene with the EML4 gene, resulting in the EML4-ALK fusion protein. This fusion protein is constitutively active, meaning it is always "on," sending continuous signals for the cancer cells to grow and divide.
Crizotinib functions as an ALK inhibitor. By binding to the ATP-binding site of the ALK protein, Crizotinib blocks its kinase activity. This inhibition prevents the phosphorylation of downstream signaling molecules that are necessary for the cancer cells to proliferate and survive.
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Lorlatinib, Capmatinib Hydrochloride Hydrate, Brigatinib