[CAS NO. 130018-87-0] Levocetirizine dihydrochloride

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PRODUCTS SPECIFICATIONS [130018-87-0]

Catalog

HY-W010841

Brand

MCE

CAS

130018-87-0

DESCRIPTION [130018-87-0]

Overview

MDL	MFCD07366507
Molecular Weight	461.81
Molecular Formula	C21H27Cl3N2O3
SMILES	O=C(O)COCCN1CCN([C@@H](C2=CC=C(Cl)C=C2)C3=CC=CC=C3)CC1.[H]Cl.[H]Cl

For research use only. We do not sell to patients.

Summary

Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria ^[1] .

In Vivo

Levocetirizine (0.4 mg/kg; oral administration; male Sprague-Dawley rats) treatment shows that the C _max , AUC _0-t , AUC _0-∞ and t _1/2 are 0.34 μg/mL, 3.26 μg h/mL, 3.67 μg h/mL and 2.34 hours, respectively in Sprague-Dawley rats ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	30 male Sprague-Dawley rats (8 weeks old; 200-250 g) ^[1]
Dosage:	0.4 mg/kg
Administration:	Oral administration (Pharmacokinetic Analysis)
Result:	The C _max , AUC _0-t , AUC _0-∞ and t _1/2 were 0.34 μg/mL, 3.26 μg h/mL, 3.67 μg h/mL and 2.34 hours, respectively.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00160680	UCB S.A. - Pharma Sector\|UCB Pharma	Rhinitis, Allergic, Perennial	March 1, 2005	Phase 4
NCT00521131	UCB Pharma	Rhinitis\|Allergic\|Perennial	September 2002	Phase 4
NCT00525382	UCB Pharma	Urticaria	August 2003	Phase 3
NCT00521170	UCB Pharma	Allergy	November 2004	Phase 1
NCT03590912	Lumbini Medical College	Otitis Media With Effusion	September 5, 2018	Phase 4
NCT04699604	Children´s Mercy Hospital Kansas City\|National Institutes of Health (NIH)	Allergic Asthma	April 28, 2021	Phase 3
NCT01430260	Handok Inc.\|Takeda	Allergic Rhinitis	January 2011	Phase 4
NCT00359138	Organon and Co	Hypersensitivity	February 2006	Phase 4
NCT00542607	UCB Pharma	Rhinitis, Allergic, Seasonal	September 2002	Phase 4
NCT00160537	UCB Pharma	Seasonal Allergic Rhinitis	May 2005	Phase 4
NCT00439712	Institut für Atemwegsforschung GmbH\|UCB Pharma	Perennial Allergic Rhinitis	February 2007	Phase 4
NCT01722162	Washington University School of Medicine	Colorectal Neoplasms	April 2013	Phase 2
NCT00355771	Institut für Atemwegsforschung GmbH\|UCB Pharma	Allergic Rhinitis	June 2006	Phase 4
NCT01250652	Association Asthma, Bulgaria\|UCB Pharma	Chronic Urticaria	March 2011	Phase 4
NCT00544388	UCB Pharma	Rhinitis, Allergic, Seasonal	April 2004	Phase 3
NCT00291642	UCB Pharma	Rhinitis\|Allergic\|Seasonal	January 1, 2006	Phase 2
NCT01392859	Children´s Mercy Hospital Kansas City	Asthma\|Allergic Asthma\|Non-allergic Asthma	June 2011	Phase 2\|Phase 3
NCT01008592	Wake Forest University\|UCB Pharma\|Wake Forest University Health Sciences	Rhinitis\|Urticaria	April 2009
NCT00264303	UCB Pharma	Chronic Idiopathic Urticaria	December 2005	Phase 4
NCT00621959	UCB Pharma	Seasonal Allergic Rhinitis	March 2008	Phase 4
NCT00295022	UCB S.A. - Pharma Sector\|UCB Pharma	Rhinitis, Allergic, Seasonal	July 29, 2006	Phase 4
NCT02507635	Iuliu Hatieganu University of Medicine and Pharmacy	Allergic Rhinitis	February 2009	Phase 4
NCT00520754	UCB Pharma	Cough	December 2001	Phase 2
NCT00619801	UCB Pharma	Allergic Rhinitis\|Chronic Urticaria	March 2008	Phase 3
NCT01563081	GlaxoSmithKline	Rhinitis	April 2012	Phase 3
NCT01557439	IPCA Laboratories Ltd.	Fasting State	February 2012	Phase 1
NCT03371849	Hanmi Pharmaceutical Company Limited	Healthy	July 19, 2017	Phase 1
NCT01445262	GlaxoSmithKline	Rhinitis, Allergic, Perennial and Seasonal	February 2011
NCT00160563	UCB Pharma	Asthma	June 2004	Phase 3
NCT03545464	Assistance Publique - Hôpitaux de Paris	Urticaria\|Angi?dema	September 21, 2019	Phase 3
NCT00160589	UCB Pharma	Rhinitis, Allergic, Perennial	April 2005	Phase 4
NCT00524836	UCB Pharma	Rhinitis\|Allergic\|Perennial	September 2003	Phase 3
NCT00152412	UCB Pharma	Allergic Rhinitis	June 2004	Phase 2
NCT03555890	GlaxoSmithKline\|Zensei Pharmaceutical Co., Ltd.	Rhinitis	May 18, 2018	Phase 1
NCT01062139	HK inno.N Corporation	Perennial Allergic Rhinitis	October 2009	Phase 4
NCT01509209	Hanmi Pharmaceutical Company Limited	Vasomotor Rhinitis	May 2011	Phase 3
NCT00679250	Brian J Lipworth\|University of Dundee	Allergic Rhinitis	November 2005	Phase 4
NCT00152464	UCB Pharma SA\|UCB Pharma	Dermatitis, Atopic	March 20, 2002	Phase 3
NCT01000792	Clinical Research International Limited	Allergic Rhinitis	November 2009	Phase 3
NCT00521040	UCB Pharma	Rhinitis, Allergic, Seasonal	February 2004	Not Applicable
NCT00789152	Organon and Co	Allergic Rhinitis	December 1, 2003	Phase 3
NCT02447393	GlaxoSmithKline	Dermatitis	March 18, 2008	Phase 1
NCT03789422	University Hospital, Grenoble	Chronic Spontaneous Urticaria	December 10, 2019	Phase 4
NCT00315523	UCB Pharma	Rhinitis, Allergic, Seasonal	July 2006	Phase 3
NCT00884325	Derm Research, PLLC\|UCB Pharma	Atopic Dermatitis\|Pruritus	February 2009	Phase 4
NCT00525278	UCB Pharma	Rhinitis\|Allergic\|Seasonal	August 2003	Phase 3
NCT01506076	Dr. Reddy´s Laboratories Limited	Fasting	December 2007	Phase 1
NCT00150761	UCB Pharma	Anti-allergic Agents	July 2004	Phase 4
NCT00421109	Faes Farma, S.A.	Urticaria	July 2006	Phase 3
NCT00375713	UCB Pharma	Dermatitis\|Eczema	October 2005	Phase 3
NCT01586091	Charite University, Berlin, Germany	Pruritus\|Chronic Urticaria\|Allergic Rhinitis	February 2011	Phase 4
NCT00653224	UCB Pharma	Seasonal Allergic Rhinitis	April 2008	Phase 4
NCT01622283	GlaxoSmithKline	Rhinitis, Allergic, Perennial and Seasonal	May 2, 2012	Phase 1
NCT01567501	IPCA Laboratories Ltd.	Fed	February 2012	Phase 1
NCT01496911	Utrecht Institute for Pharmaceutical Sciences\|Royal Netherlands Navy	Healthy Volunteers	April 2012	Phase 4
NCT02372604	Hospices Civils de Lyon	Chronic Spontaneous Urticaria	July 2015	Phase 3
NCT05348148	Camillians Saint Mary´s Hospital Luodong	Allergic Rhinitis\|Vasomotor Rhinitis	June 16, 2020	Not Applicable
NCT01491503	Hanmi Pharmaceutical Company Limited	Healthy	November 2011	Phase 1
NCT04399525	Universitaire Ziekenhuizen KU Leuven	Pruritus	October 28, 2019	Not Applicable
NCT01640535	Hanmi Pharmaceutical Company Limited	Perennial Allergic Rhinitis	June 2012	Phase 3
NCT01506063	Dr. Reddy´s Laboratories Limited	Healthy	January 2008	Phase 1
NCT00628108	UCB Pharma	Allergic Rhinitis\|Chronic Urticaria	March 2008	Phase 3
NCT00894231	AAADRS Clinical Research Center\|UCB Pharma	Perennial Allergic Rhinitis	January 2009	Phase 4
NCT00826943	Vanderbilt University	Allergic Rhinitis	January 2009	Phase 4
NCT05565729	Eli Lilly and Company\|Nektar Therapeutics	Healthy	October 5, 2022	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

H ₂ O : 100 mg/mL ( 216.54 mM ; Need ultrasonic)

DMSO : 100 mg/mL ( 216.54 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1654 mL	10.8270 mL	21.6539 mL
5 mM	0.4331 mL	2.1654 mL	4.3308 mL
10 mM	0.2165 mL	1.0827 mL	2.1654 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 50 mg/mL (108.27 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Lohar P, et al. Simultaneous bioanalysis and pharmacokinetic interaction study of acebrophylline, levocetirizine and pranlukast in Sprague-Dawley rats. Biomed Chromatogr. 2019 Dec;33(12):e4672.

Synonyms

Acetic acid, 2-[2-[4-[(R)-(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-, hydrochloride (1:2)

Acetic acid, [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-, dihydrochloride, (R)-

Acetic acid, [2-[4-[(R)-(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-, dihydrochloride

Levocetirizine dihydrochloride

Xusal

Xyzal

Xyzall

UCB 28556

(R)-Cetirizine dihydrochloride

(R)-(-)-Cetirizine hydrochloride

Allercet

Lezyncet

Allear