science

Gusperimus

Gusperimus 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 Gusperimus rather than just read about it. In short: Gusperimus is an immunosuppressive drug. It is a derivative of the naturally occurring HSP70 inhibitor spergualin, and inhibits the interleukin-2-stimulated maturation of T cells to the S and G2/M phases and the polarization of the T cells into IFN-gamma-secreting Th1 effector T cells, resulting in the inhibition of growth of activated naive CD4 T cells.

Key takeaways

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

Reference excerpt

Gusperimus is an immunosuppressive drug. It is a derivative of the naturally occurring HSP70 inhibitor spergualin, and inhibits the interleukin-2-stimulated maturation of T cells to the S and G2/M phases and the polarization of the T cells into IFN-gamma-secreting Th1 effector T cells, resulting in the inhibition of growth of activated naive CD4 T cells. Gusperimus was developed by Bristol-Myers Squibb. Currently, it is manufactured and sponsored for use as an orphan drug and for clinical studies by the Japanese company Euro Nippon Kayaku. The patent claim (see quotation) is that Gusperimus may be useful for a variety of hyperreactive inflammatory diseases such as autoimmune diseases. The drug is available in vials containing 100 mg each. There is little information about the pharmacokinetic properties of gusperimus.

Overview The European Commission assigned orphan drug status to Gusperimus in 2001 for the treatment of granulomatosis with polyangiitis, a serious form of vasculitis frequently associated with permanent disability and/or fatal outcome. There have been many cases of patients resistant to all forms of usual treatment responding very well to Gusperimus. It has been proposed that gusperimus may benefit patients with the neurological disease amyotrophic lateral sclerosis (ALS or Lou Gehrig's disease). ALS causes permanent motor deficits and disabilities up to the point that almost all motor functions, including breathing and bladder control, are lost. Patients usually have no intellectual impairments. Currently, there are no results from controlled studies in ALS patients. There have also been positive and negative anecdotal reports in patients with multiple sclerosis. As with ALS, there are no sufficient studies in MS patients. Gusperimus may possibly be of use in more common diseases and conditions such as rheumatoid arthritis, Crohn's disease, lupus erythematosus, and the prevention and therapy of transplant rejection or graft-versus-host disease.

Adverse effects Currently, only provisional and preliminary data about side-effects is available. The following side-effects have been noticed so far:

Dysgeusia (abnormal or bad taste) Drug induced leukopenia (very common) Significant infections related to therapy. It is not known if therapy with gusperimus may increase the risk of malignant diseases (lymphoma, leukemia, solid tumors), as is the case with other highly potent immunosuppressant agents such as ciclosporin or tacrolimus.

Interactions There has been little experience about clinically relevant interactions. These might be:

Other immunosuppressant drugs : Risk of infections increased. Myelotoxic drugs like 6-Mercaptopurin : Risk of serious bone marrow damage increased. Certain NSAIDs : Increased risk of hepatotoxic reactions.

Dosage Gusperimus is used in therapeutic cycles. The daily dose and the length of each cycle as well as the length of the treatment free interval depend on the degree of leukopenia/neutropenia caused by gusperimus. It is recommended to obtain complete WBC (White Blood Cell) counts during and after each cycle frequently.

Synonyms 2Common references are:

(+−)-15-Deoxyspergualin, 1-Amino-19-guanidino-11-hydroxy-4,9,12-triazanonadecane-10,13-dione, 15-Deoxyspergualin, 15-Deoxyspergualin Hydrochloride, 7-{(Aminoiminomethyl)amino]-N-[2-[[4-[(3-aminopropyl)amino]butyl]amino]]-1-hydroxy-2-oxoethyl]heptanamide, Gusperimus (Trihydrochloride), N-[[[4-[(3-Aminopropyl)amino]-butyl]carbamoyl]hydroxymethyl]]-7-guanidinoheptanamide, Spanidin

Synthesis

The BOC derivative of 4-aminobutanol is oxidized with Collins reagent to afford the aldehyde. Condensation with the ylide obtained from reaction of 3-triphenylphosphonium propionic acid with lithium hexamethyldisilazane leads to the chain extended acid. The carboxylic acid is then activated by conversion to its N-hydroxysuccinimide ester; That group is displaced by ammonia to give the corresponding amide and the BOC group is removed by acid to give the intermediate. Treatment of the aminoamide with 1-amidino-3,5-dimethylpyrazole leads to an exchange of the amidine function and formation of the corresponding guanidine. The saturated guanidino-amide is obtained by catalytic hydrogenation. Amides are well known to participate in the formation of carbinolamines and aminals. Reaction with the glyoxilamide from spermidine (shown as its hydrate) leads to displacement of one of the hydroxyl groups and formation of the corresponding carbinolamine, gusperimus.

References

https://web.archive.org/web/20120204123305/http://www.bizbozos.com/nci_Gusperimus http://ec.europa.eu/enterprise/pharmaceuticals/register/o034.htm https://web.archive.org/web/20060109201017/http://www.als.net/research/treatments/treatmentDetail.asp?treatmentID=858 "Gusperimus: Leucopenia, infection, dysgeusia: 3 case reports". Reactions Weekly. 1 (1080): 13. 2005.

Worked examples

Example 1 — a first encounter with Gusperimus

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

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

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

Frequently asked questions

What is Gusperimus in simple terms?

Why does Gusperimus 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 Gusperimus?

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 Gusperimus.