While cancer is, without a doubt, a disease of damaged DNA, scientists have, in recent years, come to the conclusion that it is not only that. In other words, they have figured out that there is more to it. Such as, for example, miscommunication inside our genes, given that it definitely plays a role in cancer development, growth, progression, as well as the treatment process. What this means that the issues is not always in broken genes. Instead, the issue can sometimes be in the silencing of genes, or their turning off at the wrong time.
So, instead of directly changing DNA, scientists have now starting to search for ways to control how genes are read and expressed. In other words, they are developing drugs that can do that, and HDAC inhibitors are among the most important ones. Now, there are various HDAC inhibitors, but Entinostat (MS-275) seems to be standing out nowadays. It is actually an oral drug that targets specific HDAC enzymes, and that is actually showing promising effects in cancer therapy, used both alone and in combination with some other therapies.
Here is a bit more about it: https://www.sciencedirect.com/topics/medicine-and-dentistry/entinostat
Given that you are here, there is no doubt that you want to understand this particular drug better. And that is, without a doubt, a good thing. So, if you’re ready to learn, you should keep on reading, because we will cover the topic of Entinostat (MS-275) HDAC inhibitor in more details, explaining what it is, how it works, as well as what its advantages actually are. This way, you will get a much clearer understanding of it all, which is ultimately what you want. Without any further ado, thus, let us start digging into the topic.
What Are HDACs and Why Do They Matter?
If you’ve been expecting to dive right into the topic of Entinostat (MS-275) HDAC inhibitor, then the expectation was a bit, well, wrong. Why? Because, clearly, to understand this drug, you have to first make sure you understand HDACs in general. So, that is the topic we are going to begin with. That is the question that we are going to answer first.
First of all, you should know that every cell in your body contains the same DNA, but that not every gene is active in every cell at the same time. Depending on what specific cells have to do, some genes will be on, and some will be kept off. And, the way DNA is packaged around histones, which are proteins, affects the way this gene activity is controlled. When DNA is wrapped tightly around the histones, genes are turned off, and when it is wrapped loosely, genes are turned on. That is the simplest explanation.
Moving on, histones can be chemically modified in different ways, and one of the methods of their modification is known as acetylation, which is basically the addition of those small chemical groups that are called acetyl groups. So, when histones are acetylated, DNA loosens up, and gene expression increases. On the other hand, when histones are deacetylated, DNA tightens, and gene expression decreases. And, HDAC, that is histone deacetylases, actually remove the acetyl groups, thus turning the genes off.
Understanding HDACs is important, because, in some cancer types, they can become overactive. This leads to silencing those genes that would normally suppress tumors or regulate their growth. So, through blocking HDACs, scientists can sometimes succeed to reactivate those genes that can suppress tumors, and thus restore the body’s natural defense mechanisms.
What Is Entinostat (MS-275) HDAC inhibitor?
This brings us to our next question. What exactly is Entinostat (MS-275) HDAC inhibitor, then? Well, to cut right to the chase, this is a drug that is designed to block those HDACs that we have explained above, which can then lead to the re-activation of some important genes that can help the body fight off cancer much more successfully. We are talking about a pill, that is, a drug that is taken orally, and that has quite a long duration of action, which means that its effects are sure to last even after the actual drug has been cleared from the bloodstream.
This particular drug has been studied for years, in respect to a wide variety of cancers, including breast cancer, lung cancer, leukemia, lymphoma, as well as melanoma. And, apart from that, it has also been studied for its potential benefits when used in combination with immunotherapy. In short, it is one of the most versatile HDAC inhibitors that is currently being studied.
How does it work, though? Well, in short, the main job of Entinostat (MS-275) HDAC inhibitor is to block those HDAC enzymes. When that happens, histones stay acetylated, which results in the DNA remaining more open and relaxed. This can lead to the previously silenced genes to become re-activated, and many of those are often tumor suppressing genes, or cell-cycle regulators, the activation of which plays a huge role in our bodies ability to defend itself against certain conditions. When the right genes are activated, cancer cells lose their ability to divide uncontrollably, and they die.
Apart from affecting the cancer cells, Entinostat (MS-275) HDAC inhibitor affects immune cells as well. In short, it changes how they interact with tumors. More precisely, it helps our immune system fight cancer off more successfully.
What Are Its Advantages?
This particular drug comes with numerous advantages. For one thing, the pill form is quite convenient, and then there is the fact that its effects are long-lasting, which is undeniably a huge benefit as well, allowing for less frequent administration. Then, Entinostat (MS-275) HDAC inhibitor is actually more selective than some other, older HDAC inhibitors, targeting specific HDAC enzymes, instead of blocking them all, which leads to fewer side effects, as well as to more predictable outcomes. Furthermore, this drug’s ability to modify the tumor immune environment is also important. And, in the end, there is the fact that it has a great combination potential, meaning it can be used together with hormone therapy, checkpoint inhibitors, as well as chemotherapy.
