Pulaile (pemetrexed disodium for injection)
pemetrexed disodium for injection

English Name: Pemetrexed Disodium for Injection.
Chinese Pinyin: Zhu She Yong Pei Mei Qu Sai Er Na.
The main ingredient of this product is pemetrexed disodium.
Chemical name: N-{4-[2-(2-Amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl }-L-glutamate disodium.

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【Name】

Common Name: Pemetrexed Disodium for Injection

Brand Name: PULAILE

English Name: Pemetrexed Disodium for Injection

Chinese Pinyin: Zhu She Yong Pei Mei Qu Sai Er Na

【Ingredients】

The main ingredient of this product is pemetrexed disodium.

Chemical name: N-{4-[2-(2-Amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl }-L-glutamate disodium.

Chemical Structure:

Molecular formula: C20H19N5Na2O6

Molecular weight:  471.37

Excipients: mannitol, citric acid.

【Description】

This product is off-white to light yellow loose solid or powder.

【Indication】

Non-small cell lung cancer (NSCLC)

As a single agent, this product is suitable for the treatment of patients with locally advanced or metastatic, non-squamous, non-small cell lung cancer whose disease has progressed after first-line chemotherapy.

This product is not recommended for in the treatment of patients with histological squamous cell carcinoma.

Malignant pleural mesothelioma

This product is indicated, in combination with cisplatin, for the treatment of patients with inoperable malignant pleural mesothelioma. 

【Strength】 0.2 g(calculated as Pemetrexed).
【Dosage and Administration】

This product must be used under the guidance of qualified physicians with experience in the application of anti-tumor chemotherapy. This product can only be used as an intravenous infusion.

The preparation of the solution must be carried out in accordance with the instructions for "preparation of intravenous infusion solutions".

In combination with cisplatin:

Malignant pleural mesothelioma

The recommended dose of this product is 500 mg/m2 body surface area (BSA) as an intravenous infusion over 10 minutes on Day 1 of each 21-day cycle. The recommended dose of cisplatin is 75 mg/m2 BSA as an intravenous infusion over 2 hours. Cisplatin should be administered approximately 30 minutes after the end of the pemetrexed  administration on Day 1 of each 21-day cycle. Appropriate hydration regimens should be given before and/or after treatment with cisplatin (see cisplatin instructions for specific dosing recommendations).

Single-Agent:

Non-squamous NSCLC

For patients with non-small cell lung cancer who have received previous chemotherapy, the recommended dose is 500 mg/m2 BSA as an intravenous infusion over 10 minutes on Day 1 of each 21-day cycle.

Premedication and Concomitant Medications:

Vitamin Supplementation

To mitigate toxicity, patients receiving pemetrexed must be instructed to take low-dose folic acid products or multivitamins containing folic acid daily. Initiate folic acid orally once daily for at least 5 days, beginning 7 days before the first dose of pemetrexed  and continuing until 21 days after the last dose of pemetrexed . Administer vitamin B12, 1 mg intramuscularly, 1 week prior to the first dose of Pemetrexed and every 3 cycles thereafter. Subsequent vitamin B12 injections may be given the same day as treatment with Pemetrexed. In clinical trials, the folic acid dose ranged from 350 to 1000 μg and the vitamin B12 dose was 1000 μg. The most commonly used oral folic acid dose in clinical trials is 400 μg. [see Warnings and Precautions].

Corticosteroids

The incidence of rash is more common in patients who are not pre-administered with corticosteroids. Pre-administration of dexamethasone (or a similar drug) can reduce the incidence and severity of skin reactions. In clinical trials, administer dexamethasone 4 mg orally twice daily for three consecutive days, beginning the day before each pemetrexed administration. [see Warnings and Precautions].

Recommendations for laboratory monitoring and dosage modifications 

Monitor

All patients receiving pemetrexed should undergo a complete blood count test, including platelet counts. The patient's minimum value and recovery should be monitored. In clinical trials, tests were performed before each dose and on days 8 and 15 of each cycle. Regular biochemical tests should be also performed prior to each dose to assess renal function and liver function. Only when the absolute neutrophil count (ANC) ≥ 1500 cells / mm3, platelet count ≥ 100,000 cells / mm3, creatinine clearance ≥ 45 mL / min, total bilirubin ≤ 1.5 times the upper limit of normal, alkaline phosphatase (AP), aspartate aminotransferase (AST or SGOT) and alanine aminotransferase (ALT or SGPT) ≤ 3 times the upper limit of normal, the patient can start treatment in the next cycle. If the tumor involves the liver, alkaline phosphatase, AST and ALT ≤ 5 times the upper limit of normal is acceptable. [see Warnings and Precautions]

Dosage Modifications

At the beginning of the next treatment cycle, dosage modifications should be made based on the lowest blood count and the most severe non-hematologic toxicity of the previous treatment cycle. In order to obtain adequate recovery time, treatment can be delayed. Upon recovery, the patient should be re-treated according to the guidelines in Tables 1-3. The guidelines in Tables 1-3 apply to dosage modifications for pemetrexed in monotherapy or in combination with cisplatin. 

2005: First-to-market generic drug in China

2007: Included in the National Torch Program by the PRC Ministry of Science and Technology

2012: National Science and Technology Major Project

2013: WIPO-SIPO Award for Chinese Outstanding Patented Invention & Industrial Design

2017: Included in NRDL