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Dolasetron mesylate hydrate (MDL-73147EF hydrate; MDL-73147) is a potent serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.
Dolasetron (MDL-73147) is a first-generation 5-hydroxytryptamine-3 (5-HT₃) receptor antagonist used for the prevention of chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting. It is administered intravenously or orally and exerts its antiemetic effects by selectively blocking serotonin binding to 5-HT₃ receptors in the gastrointestinal tract and central nervous system. While dolasetron is effective in controlling acute CINV (within the first 24 hours after chemotherapy), clinical studies have demonstrated that it is less effective than second-generation agents such as palonosetron in preventing delayed CINV (24–120 hours post-chemotherapy). Due to safety concerns regarding dose-dependent QTc interval prolongation and an increased risk of cardiac arrhythmias, the use of intravenous dolasetron has been restricted or discontinued in many clinical settings. [1,2]| Targets |
5-Hydroxytryptamine-3 Receptor Antagonist (5-HT₃ RA). Dolasetron is a first-generation 5-HT₃ receptor antagonist used for the prevention of chemotherapy-induced nausea and vomiting (CINV). [1,2]
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| ln Vitro |
Dolasetron is a first-generation 5-HT₃ receptor antagonist that prevents chemotherapy-induced nausea and vomiting (CINV) by blocking serotonin binding to 5-HT₃ receptors in the gastrointestinal tract and central nervous system. [2]
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| ln Vivo |
Clinical Efficacy – Phase III Trials: In a pooled analysis of four phase III randomized, double-blind trials, dolasetron (100 mg IV) was evaluated in patients receiving moderately emetogenic chemotherapy (MEC). The complete response (CR) rate (no emesis and no rescue antiemetics) for dolasetron in the delayed phase (>24–120 h) was 45% (pooled across older 5-HT₃ RAs), which was significantly lower than the 57% CR rate observed with palonosetron (P < 0.0001). Similarly, the overall CR rate (0–120 h) was 40% for older 5-HT₃ RAs versus 51% for palonosetron (P < 0.0001). [2]
Clinical Efficacy – Retrospective Claims Analysis: In a retrospective database analysis of 26,974 patients receiving single-day emetogenic chemotherapy, dolasetron was among the 5-HT₃ RAs evaluated. The overall delayed CINV rate at cycle 1 was 15.6%, with dolasetron showing a rate of 17.3%. Compared to palonosetron, patients receiving dolasetron had higher odds of delayed CINV in cycle 2 (odds ratio [OR] = 1.65; 95% CI: 1.27–2.15; P = 0.002). This trend continued through subsequent cycles, though not all ORs reached statistical significance. Over 6 cycles of chemotherapy, dolasetron was associated with an additional $148,960 in CINV-related charges compared to palonosetron. [1] Clinical Safety: The incidence of treatment-related adverse events (AEs) with dolasetron was 27.5% (pooled across older 5-HT₃ RAs), similar to palonosetron 0.25 mg (20.0%) and 0.75 mg (26.5%). The most common treatment-related AEs were constipation (9.2%) and headache (7.4%). [2] |
| Animal Protocol |
We analyzed patient-level data derived from four randomized, double-blind, phase III studies that compared palonosetron at doses of 0.25 mg or 0.75 mg against ondansetron 32 mg, dolasetron 100 mg, or granisetron 40 μg/kg. The primary endpoints comprised complete response (CR), defined as no emesis and no use of rescue antiemetics, during the acute (0–24 h), delayed (>24–120 h), and overall (0–120 h) phases following chemotherapy. Additional endpoints included complete control (CC), characterized by no emesis, no rescue antiemetics, and no more than mild nausea, the number of emetic episodes, and the severity of nausea.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Information regarding the use of dolasetron during lactation is limited. Until more data becomes available, caution should be exercised when using dolasetron during lactation. Alternative medications may be considered. ◉ Effects on Breastfed Infants A double-blind study randomized 160 women undergoing elective cesarean section with spinal anesthesia to two groups. One group received patient-controlled intravenous analgesia (PCA) with sufentanil (standard treatment), while the other group received PCA with dexmedetomidine in addition to standard treatment. Dexmedetomidine was administered at a dose of 5 mcg/kg, followed by a continuous infusion at a rate of 0.5 mcg/kg/hour until the end of the procedure. The latter group received PCA with dexmedetomidine in combination with sufentanil for 2 days post-operatively. Both groups received 25 mg of dolasetron in their PCA solution, and all mothers breastfed. Both groups of newborns had good behavioral and neurological assessments on postpartum days 1 and 2. [1] ◉ Effects on lactation and breast milk A double-blind study randomized 160 women undergoing elective cesarean section under spinal anesthesia to two groups: one group received patient-controlled intravenous analgesia (PCA) with sufentanil (standard treatment), and the other group received PCA with dexmedetomidine in addition to standard treatment. The dose of dexmedetomidine was 5 mcg/kg, followed by a continuous infusion at a rate of 0.5 mcg/kg/hour until the end of the surgery. The latter group received dexmedetomidine in combination with PCA with sufentanil on postoperative day 2. Both groups had 25 mg of dolasetron added to their PCA solution. Patients treated with dexmedetomidine had a shorter time to first lactation (28 hours vs 34 hours), achieved exclusive breastfeeding more quickly (8 days vs 11 days), and had more milk production on the second postpartum day. [1] |
| References |
[3]. Long-term Use of Ondansetron, Dolasetron and Granisetron for the Prevention of Nausea and Vomiting: A Review of the Clinical Effectiveness and Safety [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2014 Apr 23. Available from http://www.ncbi.nlm.nih.gov/books/NBK269203/ PubMed PMID: 25610941. |
| Additional Infomation |
Dolasetron mesylate is an indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, dolasetron mesylate competitively blocks the action of serotonin on 5-HT3 receptors, thereby inhibiting nausea and vomiting induced by chemotherapy and radiotherapy. (NCI04)
See also: Dolasetron mesylate (note moved to). |
| Molecular Formula |
C20H26N2O7S
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|---|---|
| Molecular Weight |
438.4946
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| Exact Mass |
438.146
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| Elemental Analysis |
C, 54.78; H, 5.98; N, 6.39; O, 25.54; S, 7.31
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| CAS # |
878143-33-0
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| Related CAS # |
Dolasetron;115956-12-2;Dolasetron Mesylate;115956-13-3
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| PubChem CID |
6918119
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| Appearance |
White to off-white solid powder
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| Melting Point |
178 °C
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| LogP |
2.634
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
627
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CS(=O)(=O)O.C1[C@@H]2CC(C[C@H]3N2CC(=O)C1C3)OC(=O)C4=CNC5=CC=CC=C54.O
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| InChi Key |
QTFFGPOXNNGTGZ-RCSCTSIBSA-N
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| InChi Code |
InChI=1S/C19H20N2O3.CH4O3S.H2O/c22-18-10-21-12-5-11(18)6-13(21)8-14(7-12)24-19(23)16-9-20-17-4-2-1-3-15(16)17;1-5(2,3)4;/h1-4,9,11-14,20H,5-8,10H2;1H3,(H,2,3,4);1H2/t11?,12-,13+,14?;;
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| Chemical Name |
methanesulfonic acid;[(3S,7R)-10-oxo-8-azatricyclo[5.3.1.03,8]undecan-5-yl] 1H-indole-3-carboxylate;hydrate
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| Synonyms |
878143-33-0; MDL-73147EF hydrate; Dolasetron mesylate hydrate; DOLASETRON MESYLATE; MDL73147EF hydrate; Dalasetron (Mesylate hydrate); DOLASETRON MESYLATE MONOHYDRATE;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~570.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2806 mL | 11.4028 mL | 22.8055 mL | |
| 5 mM | 0.4561 mL | 2.2806 mL | 4.5611 mL | |
| 10 mM | 0.2281 mL | 1.1403 mL | 2.2806 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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