Anti-Cancer

Quinazoline derivatives viz., Gefitinib(iressa) (Chemical name: 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholin)propoxy] and Erlotinib (tarceva) (chemical name: 4-(3-ethynylphenylamino)-6,7-(bis-2-methoxy ethoxy)-quinazoline) are molecules approved recently by US FDA for treatment against locally advanced or metastatic non-small cell lung cancer (NSCLC). These molecules inhibit tyrosine kinase associated with the epiderman growth factor receptor (EGFR-TK) We have developed patent non-infringing routes and protected the processes by filing national and international patents. These processes have several advantages viz., reduction in number of synthetic steps, improvement in yields and more economical. They are ready for commercialization/ technology transfer

Gefitinib(Iressa):
  1. It is an anti-cancer agent currently in the market, first deveveloped by Astra-Zeneca and is approved by US FDA in the year 2003.
  2. Gefitinib inhibits tyrosine kinases associated with the epidermal growth factor receptor (EGFR-TK)
  3. It is an anilinoquinazoline with the chemical name 4-Quinazolinamine, N-(3- chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholin)propoxy] having the molecular formula C22H24ClFN4O3
  4. We have developed patent non imfringing routes to make this molecule and is ready for commercialization/technology transfer.
  5. This is currently manufactured and formulated by NATCO of Hyderabad in India.
Advatnages of our processes are
  • a) Reduction in number of synthetic steps
  • b) Improvement in yields
  • c) More economical
Patents filed by VMSRF:
  1. Indian Patent application No. 1227/CHE/2005A, Publication Dated: 9th June 2006. Patent No.243575 granted on 27th October 2010.
  2. Indian Patent application No. 901/CHE/2006A. Publication Dated:30th June 2006. Patent No.236840 granted on 25th Nov 2009.
  3. Indian Patent application No. 903/CHE/2006A. Publication Dated: 30th June 2006, Patent No.236843 granted on 25th Nov 2009
Erlotinib ( Tarceva):
  1. It is an oral anti-cancer drug developed by OSI Pharmaceuticals,Genentech and Roche. It is approved by US FDA in November 2004
  2. It is used for treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC).
  3. Itís chemical name is 4-(3-ethynylphenylamino)-6,7-(bis-2-methoxy ethoxy)-quinazoline.
  4. We have developed patent noninfringing routes to synthesize this molecule and it is ready for scaled up.
  5. This molecule is not manufactured in India as of now. However Roche is selling formulations in India.
Advatnages of our processes are
  • a)Reduction in number of synthetic steps
  • b)Improvement in yields
  • c)More economical
Patents filed by VMSRF:
  1. Indian Patent application No. 1227/CHE/2005. Publication Dated: 9th June 2006.
  2. Indian Patent application No. 902/CHE/2006A. Publication Dated: 30th June 2006, Patent No. 236842 granted on 25th Nov 2009
  3. Indian Patent application No. 904/CHE/2006A. Publication Dated: 30th June 2006, Patent No. 236844 granted on 25th Nov 2009
PCTs filed by VMSRF
  1. PCT Application no.PCT/IN07/000100 filed on 12th March 2007
  2. PCT Application no.PCT/IN07/000101 filed on 12th March 2007