chemistry

Zaurategrast

Zaurategrast is a chemistry 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 Zaurategrast rather than just read about it. In short: Zaurategrast (CDP323) is a small-molecule prodrug antagonist of the vascular cell adhesion molecule 1 (VCAM-1) binding to α4-integrins. It was originally developed by the British biopharmaceutical company Celltech plc.

Key takeaways

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

Reference excerpt

Zaurategrast (CDP323) is a small-molecule prodrug antagonist of the vascular cell adhesion molecule 1 (VCAM-1) binding to α4-integrins. It was originally developed by the British biopharmaceutical company Celltech plc. (now UCB S.A.) and was a putative new drug for oral treatment of multiple sclerosis. In October 2006, UCB and Biogen Idec announced a collaboration to jointly develop and commercialize zaurategrast for the treatment of multiple sclerosis and other potential indications. In June 2009, development of zaurategrast was discontinued due to discouraging results of a Phase II clinical trial.

Mechanism of action The mechanism of action of zaurategrast were believed to rely on preventing immune cells to migrate from blood vessels through the vessel walls to reach various inflamed tissues, including the brain. This mechanism is thought to prevent overshooting immune reactions and subsequent tissue damage as seen during uncontrolled immune cell migration as in multiple sclerosis. Zaurategrast has the same mechanism of action as the monoclonal antibody natalizumab.

Results in animal models Zaurategrast was investigated in chronic experimental autoimmune encephalomyelitis (EAE) in mice. The drug was effective when given prophylactically (i.e., before the disease was induced in mice) and when given therapeutically (i.e., after outbreak of the disease) and reduced the disease severity significantly.

Clinical development The safety, tolerability, and pharmacokinetic profile of zaurategrast have been evaluated in 75 female and male healthy volunteers in three separate Phase 1 studies. Zaurategrast was well tolerated at oral doses up to 1000 mg given twice daily for 7 consecutive days with an adverse event profile comparable to that observed with placebo. There was no gender effect. The oral administration resulted in inhibition of VCAM-1 binding which could be maintained throughout a 12‑ or 24‑hour dose interval at well tolerated doses A Phase 2 study commenced in June 2007 in Europe and in the US. The study intends to enroll over 200 patients with relapsing MS who have failed earlier treatment with an interferon-beta and will compare two doses of the drug to placebo over a period of six months. The results are expected by the end of 2008., Preliminary interim efficacy analysis showed that patients enrolled in this clinical trial did not benefit as expected from zaurategrast compared to placebo after a six-month treatment period. No cases of progressive multifocal leukoencephalopathy were noted.

References

External links Listings in the US NIH trial registry

Illustrations

Worked examples

Example 1 — a first encounter with Zaurategrast

Start with the simplest possible case. Write down what Zaurategrast claims or describes in one sentence, then invent the smallest concrete situation in which that sentence is true. In chemistry, 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 Zaurategrast 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 Zaurategrast 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 Zaurategrast

In research: Zaurategrast appears in chemistry 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 Zaurategrast 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: Zaurategrast is common in secondary-school and first-year university syllabi. It links to neighbouring topics Abandoned drugs, Cyclobutenes, Immunosuppressants, so understanding it makes those chapters shorter.
In everyday life: Look for Zaurategrast 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 Zaurategrast in 20 minutes

Read the reference excerpt below once, without taking notes.
Close the page and write down what Zaurategrast 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 Zaurategrast out loud to somebody else — or to Teacher Smith in the lgStudy chat.

Frequently asked questions

What is Zaurategrast in simple terms?

Why does Zaurategrast matter?

Because it connects several chemistry 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 Zaurategrast?

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 Zaurategrast.