What are tkis?

When you think of the word ‘TKI’, what comes to mind? Perhaps it’s some sort of acronym that stands for “The Key Ingredient”? Or maybe it’s a newfangled type of cookie – like, I don’t know, Triple Kreamsicle Inventions or something? (Yum…)

Well folks, today we’re here to set the record straight once and for all. Because in reality, when people talk about TKIs they’re referring to some pretty serious stuff. And nope, it ain’t cookies.

Defining TKIs

Okay okay fine… so if not cookies or key ingredients, then what on earth are these damn things?? Well my friends, prepare yourselves for a bit of science-speak: the full name is actually “Tyrosine Kinase Inhibitors”.

Got that? Tyrosine Kinase Inhibitors. Say that three times fast, I dare ya.

Now I know what you might be thinking- how can something with SUCH an intimidatingly long name even begin to sound remotely interesting?! Trust me though- despite sounding like the name of a B-list villain from Captain America or something…

…these little molecules are actually pretty darn fascinating AND amazingly helpful!

It all starts with tyrosine kinases

First thing’s first: let’s break down those cumbersome words into more digestible chunks.

You’ve got your tyrosine – which is one fancy scientific way to refer to an amino acid found within proteins – and you’ve got your kinases. A kinase is basically just any enzyme (a protein catalyst) involved in adding phosphate groups onto other molecules.

But why should we care about these two particular types of elements?
Well folks, it turns out tyrosine kinases are pretty important when it comes to the way our cells and various systems communicate with one another. They help transmit signals both within and between cells – telling them what to do, how to grow/move/etc., and even when NOT to divide (as in the case of cancer cells).

What do TKIs have to do with it?

So… where exactly do Tyrosine Kinase Inhibitors come into play?

Well as you may have guessed from the name alone (I mean really, give yourself some credit!), these little pharmacological agents work by inhibiting or blocking the activity of tyrosine kinases!

But why block them at all?

Further clarifying folks- controlled communication among your body’s many different cell types is a great thing. When things get muddled up though – like in cases of certain cancers or other disease states – these signals can become jumbled or overexpressed.

The end result? Hyperactive, out-of-control cellular growth. And depending on which type(s) of cell(s) we’re referring to here, this kind of abnormal growth can lead directly towards tumor formation!

TKIs essentially try and “hijack” that signaling process/’telephone game-style’ messaging system I mentioned earlier – preventing those pesky tyrosine kinases from actually transmitting any directives down the line! It’s like an evil plan foiled by good ol fashioned medicine!

So how exactly does a TKI work/look?

Okay okay so they sound cool (obviously) but let’s dive a bit deeper: what are some actual examples of TKIs on the market today?

Some brand names might include:
– Gleevec
– Sutent
– Tarceva
– Nexavar
…just for starters.

Each individual medication will look slightly different based off their unique design & molecular structure (basically the shape of the drug or how all its atoms are arranged) – but essentially ALL TKIs work by fitting snuggly into a specific pocket within the enzyme molecule TAKING UP SPACE-BIOTCH!

Like so:
alt text

This space-hogging interaction prevents tyrosine kinases from binding with their usual downstream targets and thereby carries out that initial blockage/inhibition- even transmitting signals NONSENSE through other pathways.
The end result? No more abnormal cellular commands going haywire and either suppressing tumor growth or slowing it to manageable levels.

So, what kind of health conditions can a TKI help treat?

Fun tidbit! Although there’s been some really amazing advances in researching how helpful these agents can be across multiple disease states… at this point in time nearly every single FDA-approved Tyrosine Kinase Inhibitor medication available is used for one main purpose: treating cancer!

As mentioned earlier, when your typical cell functioning kicks into overdrive instead (potentially due to mutations/hiccup pausin normally smooth processes) – sometimes resulting in way too much wild cellular multiplication – then something like chemotherapies and this class of small molecules may be warranted.

But as with many things promising hope to something dreaded cancerous beings, very often times treatments will come with an assortment (some worse than others) side effects such as…

Weird skin rashes/dermatologic changes

Some users experience odd dermal alterations – including rashes on places I would NEVER EVER think possible:
– neck
– palms & soles

Yup! You heard me right folks – palms &soles! Callouses might seem less awkward after using some too.

Here is further information on skin irritation caused by cancer treatments like TKIs.

Diarrhea for DAYS basically

I mean, I’m not trying to be graphic here but… yeah. It’s a thing.
Don’t worry though friends- it ain’t always painful (just.) REALLY inconvenient – and pretty much every patient using this chemical knows about the various bowel-related issues that can crop up as an unfortunate side effect!

And let’s give it up for more exciting general GI symptoms such as: bloating/cramps/nausea/vomiting/generalized gut discomfort (yum)

Blood Pressure woes

Okay so imagine this folks – you’re walking along minding your own business when all of a sudden POOF… Your blood pressure spikes super high outta nowhere!

Sound scary? Well TBH with certain types of medication who use tyrosine kinase inhibitors that scenario may end up occurring…

In fact some medications in the class need additional monitoring each time a new dose is given (aka mandatory “BP checks” which real quick to those uninitiated = getting your blood pressure taken) proving how serious these compounds are being utilized – anything created with abilities powerful enough to tamp down critical communication channels among cells also unfortunately comes with risks attached like regulation ups & downs; That BP just might be one of em’!
Also noteworthy if you have high BP before starting one of these medicines, then there likely will NOT BE any titration needed from pre-existing levels (phew!)

Various musculoskeletal pains

Gotta mention yet another set o’potential problems you might experience after taking TKIs. These might include:
– muscle cramping or weakness
– joint/muscle/bone pain

Not gonna lie: although many are still able to perform optimally with these side effects, it might make exercise challenging – an important aspect of general health and wellbeing (even in those out there battling cancer already).

Wrapping Up

Ahhhh- so much knowledge (take a deep breath)! But at the end of the day ya’ll I hope this primer on TKIs has been both helpful AND educational sarcasm wink. While they may seem super sci-fi-obtuse & confusing (trust me folks… really… science-y stuff isn’t always my forte either) when you simplify it down, easy to understand yet pretty mind-blowing stuff pops up.

Tyrosine kinase inhibitors work by disrupting over-active cellular proliferation signals that are just inviting malignant cells’ unwanted expansion. There is no one quicker pathway towards killing off mutants once being formed than halting their rapid multiplication right away!

And although within this class of medicines approved only for treating cancers like lung cancer or leukemia; promise abounds for looking into other potential therapeutic benefits = so let’s keep our fingers crossed (&hopefully unpalmar-rashed ones at that)!)

But gotta put things in perspective: As with many medical interventions – especially involving complex interactions in such an intricate system as the human body – there almost certainly will be annoying but surmountable downsides too.

Hopeful science advances are welcomed everywhere though-and impressively enough, hopefully more uses for Tyrosine Kinase Inhibitors continue emerging regularly bringing beneficial lifesaving treatments along with them!