science

Latrepirdine

Latrepirdine 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 Latrepirdine rather than just read about it. In short: Latrepirdine (INN, also known as dimebolin and sold as Dimebon) is an antihistamine drug which has been used clinically in Russia since 1983. Research was conducted in both Russia and western nations into potential applications as a neuroprotective drug to treat Alzheimer's disease and, possibly, as a nootropic, as well.

Key takeaways

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

Reference excerpt

Latrepirdine (INN, also known as dimebolin and sold as Dimebon) is an antihistamine drug which has been used clinically in Russia since 1983. Research was conducted in both Russia and western nations into potential applications as a neuroprotective drug to treat Alzheimer's disease and, possibly, as a nootropic, as well. After a major phase III clinical trial for Alzheimer's disease (AD) treatment failed to show any benefit, three other AD trials continued. Major industry-based development in this indication essentially stopped after another Phase III trial suffered the same fate in 2012. Latrepirdine failed in the phase III trial for Huntington's disease.

Uses Latrepirdine is an orally active, small molecule compound that has been shown to inhibit brain cell death in animal models of Alzheimer's disease and Huntington's disease. Research suggests it may also have cognition-enhancing effects in healthy individuals, in the absence of neurodegenerative disease pathology. However, because of negative results in human clinical trials, the drug remains unlicensed for any neurodegenerative condition.

Clinical trials

Alzheimer's disease Latrepirdine attracted renewed interest in 2009 after being shown in small preclinical trials to have positive effects on persons suffering from Alzheimer's disease. Animal studies showing potential beneficial effects on Alzheimer's disease models were shown in Russian research in 2000. Preliminary results from human trials have also been promising. In an initial six-month phase II trial, results have shown significant improvement over placebo at 12 months. Latrepirdine showed promising results in a phase III-equivalent, double-blind trial in Russia with mild–moderate stage patients. In April 2009, Pfizer and Medivation initiated a phase III trial (CONCERT study) aiming for FDA approval. In March 2010, Pfizer announced that this clinical trial failed to show any benefit for the treatment of Alzheimer's disease patients. Numerous phase III trials for AD were recruiting in 2009. In July 2009, Pfizer and Medivation announced that "latrepirdine" was to be the proposed international nonproprietary name for latrepirdine for the treatment of Alzheimer's. In March 2010, the results of a clinical trial phase III were released; the investigational Alzheimer's disease drug dimebon failed in the pivotal CONNECTION trial of patients with mild-to-moderate disease. Pfizer had paid $225 million after bidding against several pharmaceutical companies to purchase the rights to Dimebon. With CONCERT, the remaining Pfizer and Medivation Phase III trial for latrepirdine in Alzheimer's disease failed in 2012, effectively ending the development in this indication. A Cochrane meta-analysis of the three pivotal phase III efficacy trials found no significant effect of latrepirdine on cognition and function in mild-to-moderate Alzheimer's patients, though there appears to be a modest benefit for overall behavior disturbances. Latrepirdine thus failed to alter the existing pharmacologic management of Alzheimer's disease.

Huntington's disease In April 2011, latrepirdine failed in a phase III clinical trial of patients affected with Huntington's disease. The trial was sponsored by Medivation Inc. and Pfizer.

Pharmacology Latrepirdine appears to operate through multiple mechanisms of action, both blocking the action of neurotoxic beta-amyloid proteins and inhibiting L-type calcium channels, modulating the action of AMPA and NMDA glutamate receptors, and may exert a neuroprotective effect by blocking a novel target that involves mitochondrial pores, which are believed to play a role in the cell death that is associated with neurodegenerative diseases and the aging process. It also blocks a number of other receptors, including α-adrenergic, 5-HT2C, 5-HT5A, and 5-HT6. Notably, latrepirdine lacks any anticholinergic effects.

See also List of investigational agitation drugs Cerlapirdine Idalopirdine List of Russian drugs

References

Illustrations

Worked examples

Example 1 — a first encounter with Latrepirdine

Start with the simplest possible case. Write down what Latrepirdine 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 Latrepirdine 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 Latrepirdine 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 Latrepirdine

In research: Latrepirdine 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 Latrepirdine 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: Latrepirdine is common in secondary-school and first-year university syllabi. It links to neighbouring topics 5-HT2C antagonists, 5-HT5 antagonists, 5-HT6 antagonists, so understanding it makes those chapters shorter.
In everyday life: Look for Latrepirdine 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 Latrepirdine in 20 minutes

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

Frequently asked questions

What is Latrepirdine in simple terms?

Why does Latrepirdine 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 Latrepirdine?

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 Latrepirdine.