Lapatinib API Technology Transfer
Basic Information
Name: Lapatinib
Indication: Lapatinib, in combination with capecitabine, is used for the treatment of advanced or metastatic breast cancer with ErbB-2 (HER2) overexpression in patients previously treated with anthracyclines, taxanes, and trastuzumab (Herceptin).
Chemical Structure: (Not provided in text)
CAS Number: 231277-92-2
Originator: GlaxoSmithKline (GSK)
Global and Domestic Registration/Market Status:
Approved by U.S. FDA in March 2007.
Approved by EMA in June 2008.
Approved by PMDA (Japan) in April 2009.
In China, imported by GSK in 2013. Five domestic companies have filed for registration: Sichuan Kelun, Qilu Pharmaceutical, Nanjing Simcere Dongyuan Pharmaceutical, Shandong Luoxin, and Chia Tai Tianqing.
Patent Status:
Compound Patent:
Chinese Patent: 99803887.3
Filing Date: January 8, 1999
Expiry Date: January 8, 2019
Formulation Patent:
Chinese Patent: 200680021941.7
Filing Date: April 18, 2006
Expiry Date: April 18, 2026
Ditosylate Salt and Polymorph Patent:
Chinese Patent: 01812051.2
Filing Date: June 28, 2001
Expiry Date: June 28, 2021
Market Prospects
Lapatinib is a frontline treatment for metastatic breast cancer, demonstrating significant efficacy in ErbB2 (HER2)-positive advanced breast cancer, with a response rate exceeding 30% as a monotherapy, even in patients unresponsive to trastuzumab. At the June 2018 ASCO Annual Meeting, a multinational, multicenter Phase III clinical trial showed that combining lapatinib with capecitabine chemotherapy further improved treatment outcomes in ErbB2-positive advanced breast cancer, reducing the incidence of brain metastases without increasing side effects. Another study at the same meeting confirmed lapatinib’s efficacy in treating brain metastases in ErbB2-positive breast cancer, highlighting its significant clinical value for breast cancer.
Beyond breast cancer, lapatinib shows therapeutic potential in other malignancies, such as bladder cancer, kidney cancer, colorectal cancer, and lung cancer, likely due to its inhibitory effects on ErbB1 or ErbB2 tyrosine kinase activity, which is abnormally active in these tumors.
Lapatinib has minimal side effects, primarily including rash, diarrhea, and mild liver function impairment. Cardiac toxicity is rare and less severe than that of trastuzumab, with cardiac function typically recovering to normal after discontinuation.
Given its proven efficacy across multiple malignant tumors, particularly breast cancer, minimal side effects, and convenient oral administration, lapatinib offers significant clinical potential compared to traditional chemotherapy or single-target therapies. It holds promise for benefiting a broader range of cancer patients in the future.
Collaboration Model
Technology transfer, customization, etc.
