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Palonosetron Hydrochloride Injection

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Jiangsu Simcere Pharmaceutical Co., Ltd.

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Product Description

Palonosetron Hydrochloride Injection

Generic name: Palonosetron Hydrochloride Injection
Brand name: Lowvo
Composition:
The main ingredient of this product is Palonosetron hydrochloride.
Chemical name: (3aS)-2-(3S)-1-Azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1H- benz[de]isoquinolin-1
-one monohydrochloride
Chemical structure:

Palonosetron Hydrochloride Injection

Molecular formula: C19H24N2O·HCl
Molecular weight: 332.87
Description: This product is colorless and clear liquid.
Indications:
1. Prevention of acute nausea and vomiting caused by severe emetogenic chemotherapy;
2. Prevention of nausea and vomiting caused by moderate emetogenic chemotherapy;
Strength: 5mL : 0.25mg (based on C19H24N2O)
Dosage and Administration:
The recommended dose is, about 30 minutes before chemotherapy, a single intravenous dose  Palonosetron
hydrochloride 0.25mg, injection time of 30 seconds or more.
Contraindications:
Contraindicated in patients with known hypersensitivity to the drug or any component of the drug.
Precautions:
Allergic reactions may occur to patients of other selective 5-HT3 receptor antagonist allergy.
Palonosetron did not lead to clinically significant QTc interval prolongation at the dose levels studied in clinical
trials abroad. In a complete QT / QTc study of double-blind, randomized, parallel, placebo-controlled and
positive controls (moxifloxacin) in 221 healthy adult male and female volunteers, the affect of Palonosetron on
QTc interval was evaluated. The results showed that no effects on QTc interval and other ECGs were
observed at doses of 0.25 mg, 0.75 mg, 2.25 mg and no clinically significant changes in heart rate,
atrioventricular conduction and cardiac repolarization were observed neither. However, based on information
of other 5-HT3 receptor antagonist, Palonosetron should be used with caution in patients with prolonged QT
intervals and with or expected to develop QT interval prolongation. These patients include those with
hypokalemia or hypomagnesemia, patients with electrolyte abnormalities caused by taking diuretics, patients
with congenital QT syndrome, patients taking antiarrhythmic or other medications that lead to prolonged QT
intervals, and patients who have given cumulative high-dose anthracycline treatment.
Palonosetron hydrochloride injection can not be mixed with other drugs, so before and after the use of Palono-
setron hydrochloride injection, both need to apply saline flush infusion line.
Clinical studies:
The following data are mainly from foreign research literature.
In three phase III clinical studies and one phase II clinical study, the efficacy of a single dose of Palonosetron
in the prevention of acute and delayed nausea and vomiting caused by moderate and highly emetogenic che-
motherapy was evaluated. In these double-blind clinical studies, complete remission for at least 120 hr after
chemotherapy (no episodes of vomiting and no medication) and other efficacy parameters were evaluated;
and the safety and efficacy of Palonosetron in repeat chemotherapy were evaluated.
Moderate emetogenic chemotherapy
In two phase III double-blind clinical trials, clinical study case number of 1132, 30 minutes prior to moderate
emetogenic chemotherapy, volunteers were given a single intravenous dose of Palonosetron and a single
intravenous dose of Ondansetron (Study 1) and Dolasetron (Study 2). Chemotherapeutic agents used include
carboplatin ≤50 mg/m2, cyclophosphamide <1500 mg/m2, doxorubicin>25 mg/m2, epirubicin, irinotecan, me-
thotrexate>250 mg/m2. Patients in Study 1 was not given prophylactic corticosteroids. Only 4-6% of patients
in Study 2 were given corticosteroids. 77% of the patients in this study were female, 65% were caucasian and
54% were initial chemotherapy. The average age was 55 years old.
Highly emetogenic chemotherapy
In a phase II, double-blind, clinical trial, 161 patients who received initial chemotherapy received highly emet-
ogenic chemotherapy (cisplatin ≥70 mg/m2 or cyclophosphamide>1100 mg/m2) and the efficacy of a single
dose of Palonosetron 0.3-90 µg/kg (equivalent to a fixed dose of <0.1 mg-6 mg) was evaluated. Corticostero
ids were not given prophylactically. Experimental data analysis showed that 0.25 mg Palonosetron is the
lowest effective dose to inhibit acute nausea and vomiting induced by severe emetogenic chemotherapy.
In a phase III, double-blind, clinical trial involving 667 patients, a single intravenous injection of Palonosetron
or Ondansetron were performed 30 minutes prior to severe emetogenic chemotherapy (cisplatin ≥60 mg/m2,
or cyclophosphamide>1500 mg/m2, dacarbazine) , the therapeutic efficacy of Palonosetron and Ondansetron
were compared (Study 3). 67% of patients received corticosteroids prior to chemotherapy, 51% were female,
60% were caucasian, and 59% were initial chemotherapy. The average age was 52 years old.
Clinical results
Phase III clinical efficacy of Palonosetron in the prevention of acute (0-24 hr) vomiting evaluation results in
Table 1, the prevention of delayed (24-120 hr) vomiting evaluation results in Table 2, the overall (0-120 hr)
prevention of vomiting evaluation results are shown in Table 3.
Palonosetron Hydrochloride Injection
a  Number of treated cases
b  Bilateral Fisher's exact test. Significance level α = 0.025
c  Non-inferiority hypothesis tests were performed on these studies. A lower limit of -15% meets the n
on-inferiority assumption between Palonosetron and the control drug.

Studies have shown that Palonosetron is effective in preventing acute nausea and vomiting in patients who
have had initial or repeated chemotherapy with moderate or severe emetogenic. In Study 3, prophylactic
corticosteroids can enhance the efficacy. There is insufficient data to show that Palonosetron have clinical
advantages to other 5-HT3 receptor antagonists in prevention of nausea and vomiting during the acute phase.

Palonosetron Hydrochloride Injection

a  Number of treated cases
b  Bilateral Fisher's exact test. Significance level α = 0.025
c  Non-inferiority hypothesis tests were performed on these studies. A lower limit of -15% meets the
non-inferiority assumption between Palonosetron and the control drug.

Studies have shown that Palonosetron is effective in preventing delayed nausea and vomiting associated
with initial and repeated moderate emetogenic chemotherapy.

Palonosetron Hydrochloride Injection

a  Number of treated cases
b  Bilateral Fisher's exact test. Significance level α = 0.025
c  Non-inferiority hypothesis tests were performed on these studies. A lower limit of -15% meets the non-
inferiority assumption between Palonosetron and the control drug.

Studies have shown that Palonosetron is effective in preventing nausea and vomiting at 120 hr (5 days) after
initial and repeated moderate emetogenic chemotherapy.
Pharmacology and toxicology:
Pharmacology
Palonosetron is a strong affinity 5-HT3 receptor selective antagonist with no affinity or lower affinity for other
receptors. The 5-HT3 receptor is located in the vagal nerve endings in and around the emetic induction zone
in the last region of the medulla oblongata. Chemotherapeutic drugs release 5-HT by stimulating small
intestine chromaffin cells. 5-HT reactivates vagal afferent 5-HT3 receptors and produces vomiting reflexes.
Toxicology
Carcinogenicity
In a continuous 104-week carcinogenicity study of CD-1 mice, animals were orally administered Palonosetron
at doses of 10, 30, and 60 mg/kg/day. The results showed that Palonosetron was non-carcinogenic. System
exposure (plasma AUC) of Palonosetron resulting from the highest test dose was 150-289 times the human
recommended intravenous dose of 0.25 mg after exposure to Palonosetron (AUC=29.8 ng.h/mL). In a 104
-week carcinogenicity study of SD rats, male and female rats were orally administered Palonosetron at doses
of 15, 30, 60 mg/kg /d and 15, 45, 90 mg/kg/day, respectively. System exposure (plasma AUC) of
Palonosetron resulting from the highest test dose was 137-308 times that of the human recommended i
ntravenous dose. And Palonosetron results in increased incidence of benign adrenal pheochromocytoma and
benign and malignant mixtures pheochromocytoma , pancreatic islet cell adenoma, mixed adenoma and s
arcoma and pituitary tumors in male rats. And it will lead to the increased incidence of hepatocellular
adenoma and sarcoma, thyroid C-cell adenomas, mixed adenoma and sarcoma increases in female rats.
Mutagenicity
Bacterial Ames test, Chinese hamster ovary cell mutagenicity test, in vitro hepatocyte disordered DNA
synthesis (UDS) test or mouse micronucleus test showed that Palonosetron has no mutagenicity. However,
Palonosetron has a distortion effect on the chromosome of Chinese hamster ovary cells.
Reproductive toxicity
Oral administration of rat dose of 60 mg/kg (by body surface area, about 1894 times of the recommended
intravenous injection for human), did not affect fertility of male and female rats.
Pharmacokinetics:
The following data are from foreign clinical research literature.
After administration of Palonosetron to healthy volunteers and cancer patients intravenously, as the drug
slowly eliminate in the body, plasma concentration begins to decline. Mean maximum plasma concentration
(Cmax) and area under the concentration-time curve (AUC0→∞) are generally dose-proportional over the
dose range of 0.3-90 µg/kg in healthy subjects and in cancer patients. Six cancer patients were given a single
dose of Palonosetron of 3 μg/kg (or 0.21 mg/70 kg), with a maximum plasma concentration of 5.6±5.5 ng/mL
and an average AUC of 35.8±20.9 ng.hr/mL.
Following intravenous administration of Palonosetron 0.25 mg once every other day for 3 doses in 11
testicular cancer patients, the mean (± SD) increase in plasma concentration from Day 1-Day 5 was 42±34%.
After intravenous administration of Palonosetron 0.25 mg once daily for 3 days in 12 healthy subjects, the
mean (± SD) increase in plasma Palonosetron concentration from Day 1 to Day 3 was 110±45 %.
Distribution
The distribution volume of Palonosetron is 8.3±2.5L/kg, and the plasma protein binding rate is about 62%.
Biotransformation
Palonosetron is eliminated by dual route, approximately 50 % metabolised to form two primary metabolites,
which have less than 1 % of the 5HT3 receptor antagonist activity of palonosetron. In vitro metabolism studies
have shown that CYP2D6 and to a lesser extent, CYP3A and CYP1A2 isoenzymes are involved in the
metabolism of palonosetron. However, clinical pharmacokinetic parameters are not significantly different
between poor and extensive metabolisers of CYP2D6 substrates.
Elimination
A single dose of 10 μg/kg 14C Palonosetron was intravenously administered. After 144 hr, the radioactive
marker present in the urine accounted for about 80% of the administered dose, with Palonosetron about 40%
. The whole body clearance rate of healthy volunteers was 160±35 mL/h/ kg, the renal clearance rate was
66.5±18.2 mL/h/kg and the average terminal elimination half-life was 40 hours.
Elderly people
Population pharmacokinetic analysis and clinical safety and efficacy data show no difference between elderly
patients ≥65 years and young patients (18-64 years). Therefore, elderly patients do not need to adjust the dose.
Different races
Pharmacokinetic studies were performed on 24 Japanese healthy volunteers. Palonosetron administered
intravenously at a dose ranging from 3-90 μg/kg had 25% more systemic clearance than Caucasians, but did
not require dose adjustment. The melanoderm's pharmacokinetics of Palonosetron is not sufficient.
Renal impairment
Light to moderate renal impairment did not significantly affect pharmacokinetic parameters of Palonosetron,
and systemic exposure in patients with severe renal impairment increased by approximately 28% compared
to healthy volunteers. Therefore, patients with varying degrees of renal impairment do not need to adjust the
dose.
Hepatic impairment
Compared with healthy volunteers, hepatic impairment had no significant effect on the rate of systemic
clearance of Palonosetron, so no dose adjustments were needed for patients with varying degrees of hepatic
impairment.
Storage:Protect from light, and seal up.
Packs:Package material: ampoule bottle; Package size: 1 bottle/box, 2 bottle/box, 5 bottle/box.
Shelf-life:24 months