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Related Concept Videos

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists

5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
Antidepressant Drugs: MAOIs and Other Agents01:23

Antidepressant Drugs: MAOIs and Other Agents

Atypical antidepressants, including bupropion (Wellbutrin), mirtazapine (Remeron), nefazodone (Serzone), trazodone (Desyrel), and vilazodone (Viibryd), offer unique mechanisms of action. Bupropion weakly inhibits dopamine and norepinephrine reuptake, aiding depression treatment and smoking cessation, with a low risk of sexual dysfunction. Mirtazapine enhances serotonin and norepinephrine neurotransmission, leading to sedation, increased appetite, and weight gain. As a result, it helps treat...
Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists01:23

Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists

Serotonin, a crucial neurotransmitter synthesized by enterochromaffin cells, plays a cardinal role in regulating gastrointestinal (GI) motility. With over 90% of the body's total serotonin in the GI tract, its influence on digestive processes is profound. Serotonin is swiftly released upon various stimuli, such as food boluses or certain drugs, triggering intrinsic sensory neurons in the myenteric plexus and extrinsic vagal and spinal sensory neurons. This leads to the activation of the...
Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists01:29

Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists

Dopamine receptor antagonists, also known as antipsychotic agents, are critical in managing chemotherapy-induced vomiting. These antiemetic agents block dopamine receptors in the chemoreceptor trigger zone (CTZ), inhibiting signal transmission to the vomiting center. Antipsychotic agents encompass phenothiazines (PTZ), butyrophenones, benzamides, and thienobenzodiazepines (Zyprexa), which are utilized for their antiemetic and sedative properties.
Phenothiazines, such as prochlorperazine...
Drugs Affecting GI Tract Motility: Dopamine Receptor Antagonists01:28

Drugs Affecting GI Tract Motility: Dopamine Receptor Antagonists

Prokinetic agents are specialized medications that stimulate gastrointestinal (GI) motility, promoting food movement through the GI tract. Dopamine, an inhibitory neurotransmitter, plays a significant role in this process, reducing GI motility and indirectly controlling the speed of digestion. Dopamine receptor antagonists, such as metoclopramide and domperidone, offer a unique advantage as prokinetic agents. By blocking the dopamine receptors, these drugs increase GI motility, improving food...
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates these...

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Related Experiment Video

Updated: Jun 16, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
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Laromustine (cloretazine).

Norbert Vey1, Frank Giles

  • 1Unité d'Hématologie 3, Institut Paoli-Calmettes, Department of Hematology, 232 Blvd Sainte Marguerite, 13009 Marseille, France. veyn@marseille.fnclcc.fr

Expert Opinion on Pharmacotherapy
|February 19, 2010
PubMed
Summary

Laromustine shows significant activity in acute myelogenous leukemia (AML), particularly in elderly patients. While effective as a single agent, further research is needed to establish optimal dosing and safety for combination therapies in relapsed AML.

Area of Science:

  • Hematology
  • Oncology
  • Pharmacology

Background:

  • Acute myelogenous leukemia (AML) has a poor prognosis, especially in elderly and relapsed patients.
  • Current standard of care is lacking for these patient groups, highlighting the need for novel therapeutic agents.
  • Laromustine, a novel sulfonylhydrazine alkylator, has emerged as a potential treatment option.

Purpose of the Study:

  • To review preclinical and clinical studies of Laromustine in AML.
  • To summarize the mechanisms of action and supporting preclinical data for Laromustine in AML.
  • To evaluate the efficacy and toxicity of Laromustine in various AML patient populations.

Main Methods:

  • Review of published preclinical and clinical studies on Laromustine in AML (2000-2009).

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  • Analysis of Laromustine's mechanism of action and preclinical data.
  • Evaluation of Phase II and Phase III clinical trial outcomes, including response rates and toxicity profiles.

    • Main Results:

    • Laromustine demonstrated limited extramedullary toxicity.
    • Phase II studies showed a 32% complete response rate in elderly, previously untreated AML patients.
    • A Phase III study combining Laromustine with cytarabine in relapsed AML showed increased response rates but also excessive toxicity.

    Conclusions:

    • Laromustine exhibits significant activity in AML.
    • As a single agent, Laromustine may offer an alternative treatment for elderly AML patients.
    • Further investigation is required to establish the safety and optimal dosing of Laromustine in combination regimens.