science

Phosphoinositide 3-kinase inhibitor

Phosphoinositide 3-kinase inhibitor is a science topic covered in the lgStudy science library. This page brings together a partial reference excerpt, illustrations, worked examples, real-world applications and a short study plan, so you can understand Phosphoinositide 3-kinase inhibitor rather than just read about it. In short: Phosphoinositide 3-kinase inhibitors (PI3K inhibitors) are a class of medical drugs that are mainly used to treat advanced cancers. They function by inhibiting one or more of the phosphoinositide 3-kinase (PI3K) enzymes, which are part of the PI3K/AKT/mTOR pathway.

Key takeaways

Phosphoinositide 3-kinase inhibitor belongs to science; place it in that map before memorising details.
Learn the definition first, then one example that makes the definition concrete.
Connect Phosphoinositide 3-kinase inhibitor to a quantity you can measure, compute or draw — that is where exam questions come from.
Reproduce the core statement of Phosphoinositide 3-kinase inhibitor from memory before moving on to harder problems.

Reference excerpt

Phosphoinositide 3-kinase inhibitors (PI3K inhibitors) are a class of medical drugs that are mainly used to treat advanced cancers. They function by inhibiting one or more of the phosphoinositide 3-kinase (PI3K) enzymes, which are part of the PI3K/AKT/mTOR pathway. This signal pathway regulates cellular functions such as growth and survival. It is strictly regulated in healthy cells, but is always active in many cancer cells, allowing the cancer cells to better survive and multiply. PI3K inhibitors block the PI3K/AKT/mTOR pathway and thus slow down cancer growth. They are examples of a targeted therapy. While PI3K inhibitors are an effective treatment, they can have very severe side effects and are therefore only used if other treatments have failed or are not suitable. After PI3K inhibitors had been under investigation as anti-cancer drugs for several years, the first one to be approved for treatment in clinical practice was idelalisib in 2014. Several others followed, and even more are still under development (see below). There are different classes and isoforms of PI3Ks. Class 1 PI3Ks have a catalytic subunit known as p110, with four types (isoforms) – p110 alpha (PIK3CA), p110 beta (PIK3CB), p110 gamma (PIK3CG) and p110 delta (PIK3CD). All PI3K inhibitors that are currently approved inhibit one or more p110 isoforms of the class I PI3Ks. Inhibiting different p110 isoforms can have different effects, e.g. PTEN-negative tumors may be more sensitive to PIK3CB inhibitors. PI3K inhibitors are also under investigation as treatments for inflammatory respiratory disease, and are used to investigate the role of the PI3K pathway in aging.

Approved for treatment Idelalisib (trade name Zydelig; codenamed CAL-101, GS-1101; PIK3CD inhibitor): FDA-approved in July 2014 for treatment of three types of blood cancers: treatment of relapsed or refractory chronic lymphocytic leukemia (CLL) in combination with rituximab, treatment of relapsed small lymphocytic lymphoma after at least two prior systemic therapies, and treatment of follicular lymphoma (FL) after at least two prior systemic therapies. Copanlisib (trade name Aliqopa; codenamed BAY 80-6946; predominantly a PIK3CA and PIK3CD inhibitor): FDA-approved in September 2017 for treatment of relapsed follicular lymphoma after at least two prior systemic therapies. Duvelisib (trade name Copiktra; codenamed INK1197, IPI-145; PIK3CD and PIK3CG inhibitor): FDA-approved on 24 September 2018 for treatment of relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) after at least two prior therapies, and treatment of relapsed or refractory follicular lymphoma after at least two prior systemic therapies. Alpelisib (trade names Piqray and Pivikto; codenamed BYL719; PIK3CA inhibitor): FDA-approved in May 2019 for treatment of HR-positive and HER2/neu-negative breast cancer in combination with the endocrine therapy fulvestrant. Umbralisib (trade name Ukoniq; codenamed TGR-1202, Rp-5264; PIK3CD and casein kinase CSNK1E inhibitor): FDA-approved in February 2021 for treatment of relapsed or refractory marginal zone lymphoma (MZL) after at least one prior anti-CD20-based regimen, and treatment of relapsed or refractory follicular lymphoma after at least three prior lines of systemic therapy. As of May 31, 2022, umbralisib was withdrawn from the US market due to the decrement in overall survival and increased serious adverse events when using umbralisib. Leniolisib (codenamed CDZ173; PIK3CD inhibitor, trade name Joenja) was tested as a potential treatment for activated PI3K delta syndrome (APDS) / PASLI disease in a placebo-controlled phase II/III trial (NCT02435173). The trial was completed in August 2021 and results have become available in March 2022. Another phase II/III trial for APDS/PASLI that serves as an extension study (NCT02859727) is still ongoing and results are expected for October 2026. The FDA has approved leniolisib on March 24, 2023. Inavolisib (trade name Itovebi ; codenamed GDC-0077; PI3K-alpha inhibitor): FDA-approved on 10 October 2024 for treatment of PIK3CA-mutated, HR-positive, and HER2-negative breast cancer in combination with palbociclib (CDK4/6 inhibitor) and fulvestrant.

Under clinical development

Late stage In phase III clinical trials:

… excerpt ends here. Continue reading the full article.

Illustrations

Worked examples

Example 1 — a first encounter with Phosphoinositide 3-kinase inhibitor

Start with the simplest possible case. Write down what Phosphoinositide 3-kinase inhibitor claims or describes in one sentence, then invent the smallest concrete situation in which that sentence is true. In science, the smallest case is usually a single object, a single equation or a single measurement. Check that every symbol or term in your sentence has a meaning in that case.

Example 2 — changing one variable

Take the situation from Example 1 and change exactly one quantity: double it, halve it, or set it to zero. Predict what should happen to Phosphoinositide 3-kinase inhibitor before you calculate. Comparing your prediction with the result is the fastest way to find out whether you understand the idea or only the words.

Example 3 — an exam-style question

Typical questions about Phosphoinositide 3-kinase inhibitor ask you to (a) state it precisely, (b) apply it to given data, and (c) explain a limitation. Practise writing all three answers in under five minutes; the third part is what separates a full-mark answer from an average one.

Applications of Phosphoinositide 3-kinase inhibitor

In research: Phosphoinositide 3-kinase inhibitor appears in science research whenever the underlying quantities have to be modelled precisely. Papers usually cite it as a starting assumption and then explore where it breaks down.
In technology and industry: Engineering practice reuses Phosphoinositide 3-kinase inhibitor in design rules, simulations and safety margins. Knowing the idea lets you read a specification sheet and understand why the numbers look the way they do.
In the classroom: Phosphoinositide 3-kinase inhibitor is common in secondary-school and first-year university syllabi. It links to neighbouring topics Experimental cancer drugs, Phosphoinositide 3-kinase inhibitors, Targeted therapy, so understanding it makes those chapters shorter.
In everyday life: Look for Phosphoinositide 3-kinase inhibitor outside the textbook — in sport, cooking, traffic, electronics or the sky above you. An example you found yourself is remembered far longer than one you were given.

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How to study Phosphoinositide 3-kinase inhibitor in 20 minutes

Read the reference excerpt below once, without taking notes.
Close the page and write down what Phosphoinositide 3-kinase inhibitor means in your own words.
Compare your version with the excerpt and mark what you missed.
Work through the three examples above with pen and paper.
Explain Phosphoinositide 3-kinase inhibitor out loud to somebody else — or to Teacher Smith in the lgStudy chat.

Frequently asked questions

What is Phosphoinositide 3-kinase inhibitor in simple terms?

Why does Phosphoinositide 3-kinase inhibitor matter?

Because it connects several science ideas at once: it gives you a definition you can apply, a quantity you can calculate, and a way to check whether a result is plausible.

How should I study Phosphoinositide 3-kinase inhibitor?

Read the excerpt, restate it from memory, then work through the examples and applications listed on this page. The five-step study plan above takes about twenty minutes.

What does this page cover?

It gives you a compact reference excerpt plus original lgStudy explanations, examples, applications and study material on Phosphoinositide 3-kinase inhibitor.