chemistry

Lasofoxifene

Lasofoxifene 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 Lasofoxifene rather than just read about it. In short: Lasofoxifene, sold under the brand name Fablyn, is a nonsteroidal selective estrogen receptor modulator (SERM) which is marketed by Pfizer in Lithuania and Portugal for the prevention and treatment of osteoporosis and for the treatment of vaginal atrophy, and the result of an exclusive research collaboration with Ligand Pharmaceuticals (LGND). It also appears to have had a statistically significant effect of reducin…

Key takeaways

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

Reference excerpt

Lasofoxifene, sold under the brand name Fablyn, is a nonsteroidal selective estrogen receptor modulator (SERM) which is marketed by Pfizer in Lithuania and Portugal for the prevention and treatment of osteoporosis and for the treatment of vaginal atrophy, and the result of an exclusive research collaboration with Ligand Pharmaceuticals (LGND). It also appears to have had a statistically significant effect of reducing breast cancer in women according to a study published in The Journal of the National Cancer Institute.

Medical uses

Osteoporosis In postmenopausal women with osteoporosis, lasofoxifene at a dose of 0.5 mg per day was associated with reduced risks of nonvertebral and vertebral fractures, ER-positive breast cancer, coronary heart disease, and stroke but an increased risk of venous thromboembolic events.

Breast cancer In studies of breast cancer prevention, lasofoxifene showed a 79% reduction in breast cancer incidence and an 83% reduction specific incidence of estrogen receptor-positive breast cancers, which is significantly higher than reductions found with the related SERMs tamoxifen and raloxifene. In accordance, a network meta-analysis of SERMs for breast cancer prevention found the highest reduction in risk with lasofoxifene of all the drugs. The reduction was even greater than that observed with aromatase inhibitors, which have generally been found to confer a greater risk reduction than SERMs. It also has shown promise in ESR1 mutant patients with 'approximately 40% of patients harboring this mutation'.

Pharmacology

Pharmacodynamics Lasofoxifene selectively binds to both ERα and ERβ with high affinity. Its IC50 for ERα (1.5 nM) is similar to that of estradiol (4.8 nM) and is at least 10-fold higher than those of tamoxifen.

Pharmacokinetics Lasofoxifene has greatly improved oral bioavailability relative to tamoxifen and raloxifene, and this may also be involved in its greater potency.

Chemistry Lasofoxifene is a naphthalene derivative and a desmethyl dihydro analogue of nafoxidine.

History In September 2005, Pfizer received a non-approvable letter from the U.S. Food and Drug Administration regarding lasofoxifene (trade name Oporia), a selective estrogen receptor modulator for the prevention of osteoporosis. In January 2008, Ligand Pharmaceuticals, through its marketing partner, Pfizer, submitted a New Drug Application for lasofoxifene, which is expected to be marketed under the tradename Fablyn. Lasofoxifene was approved in the EU under the brand name Fablyn by the EMEA in March 2009.

Research Lasofoxifene is under development by Sermonix Pharmaceuticals for the treatment of metastatic breast cancer and dyspareunia associated with vaginal atrophy in the United States and Europe. It is also being researched for the potential treatment of ovarian cancer. As of December 2017, lasofoxifene is in phase III clinical trials for breast cancer and phase II clinical studies for dyspareunia.

See also List of investigational sexual dysfunction drugs

References

External links Lasofoxifene - AdisInsight "Reference site for lasofoxifene information". Anakena Internet Services SL. Retrieved 2008-03-18.

Illustrations

Worked examples

Example 1 — a first encounter with Lasofoxifene

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

In research: Lasofoxifene 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 Lasofoxifene 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: Lasofoxifene is common in secondary-school and first-year university syllabi. It links to neighbouring topics 1-Pyrrolidinyl compounds, Hormonal antineoplastic drugs, Hydroxyarenes, so understanding it makes those chapters shorter.
In everyday life: Look for Lasofoxifene 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 Lasofoxifene in 20 minutes

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

Frequently asked questions

What is Lasofoxifene in simple terms?

Why does Lasofoxifene 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 Lasofoxifene?

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 Lasofoxifene.