Imatinib Loss Will be Novartis Gain

Imatinib Mesylate, a revolutionary first-line therapy for chronic myelogenous leukaemia (CML) has constantly been in news for few years mostly over patent related issues involving Swiss-major Novartis, Indian Generic Companies, NGOs, and Indian Patent System and that also for its beta crystalline form. Although Novartis’s writ challenging the constitutional validity of section 3(d) had already been knocked down by the Chennai High Court, but is keen fighting against the Chennai Patent Office decision rejecting the Application No. 1602/MAS/98 for beta crystalline form of Imatinib Mesylate, which is currently pending for hearing with newly constituted Intellectual Property Appellate Board (IPAB). The Chennai High Court decision, which undoubtedly stayed away from determining the scope of section 3(d) and meaning of ‘efficacy’ came no surprise to Patent Circle, but surely will be looking forward towards IPAB decision.

Imatinib Mesylate Beta Crystalline Mail-box Application

Application Number	1602/MAS/98
Applicant	Novartis AG
Title	Crystal Modification of a N-Phenyl-2- Pyrimidineamine Derivative Processes for its Manufacture and its use
Date of Filing	July 17, 1998
Gazette Date	July 17, 1999
Convention Date	July 18, 1997
Convention	Yes

Source: Ekaswa Database, Patent Facilitating Centre, Department of Science & Technology

Unrelated from Imatinib Mesylate testing time in India, Novartis was busy discovering and conducting clinical trials for yet another breakthrough for chronic myelogenous leukaemia and subsequently obtained the US Food and Drug Administration approval for CML second-line therapy drug Nilotinib Hydrochloride Monohydrate in October last year. Globally launched as Tasigna, Nilotinib belongs to tyrosine kinase inhibitor showing therapeutic indication in patients with chronic myelogenuos leukaemia who are resistant or tolerant to Gleevac (Imatinib Mesylate). According to a press release from the University of Texas MD Anderson Cancer Center, “Nilotinib is up to 50 times more potent than Gleevec because it was designed to more efficiently bind to, and shut down, the protein enzyme responsible for the disease.” According to observation of Hagop Kantarjian, M.D., professor and chair of the Department of Leukaemia, Nilotinib seems to have fewer side effects than Gleevec. Technically, Nilotinib formerly called AMN107 during trials is a derivative of Imatinib and half of the molecule (“the working end”) is the same as Imatinib, but differing in the other half (“the trunk and tail lights”).

Although Imatinib has overall excellent survival rate and showed a remarkable ability to contain chronic myelogenous leukaemia in patients, but still not been able to cure the disease (as reported by Brian Druker, M.D. of the Oregon Health and Science University). The possibility of patients’ developing resistance to Imatinib over course of time and shifting to second-line therapy Nilotinib cannot be ruled out, which may put Nilotinib as a front-runner for the treatment of CML (watch short Nilotinib Animation). Novartis has already received the US Patent No. 7,169,791 (the ‘791) and has pending mail-box application No. 3003/CHENP/2004 with the Chennai Patent Office for Nilotinib, both claiming priorities from British Application Nos. 0215676.8 and 0229893.3. So, irrespective what will be the outcome of Imatinib beta crystalline application in India, Novartis will still gain from the Imatinib (inhibiting) loss!

Nilotinib Mail-box Application

Application Number	3003/CHENP/2004
Applicant	Novartis AG Switzerland
Title	Inhibitors of Tyrosine Kinases
Inventors	Breitenstein Werner Furet Pascal Jacob Sandra Manley Paul William
International Class	C07D
Date of Filing	December 31, 2004
Journal Date	February 17, 2006
Priority Date	July 05, 2002
Priority Country	Great Britain
Priority	Yes

Source: Ekaswa Database, Patent Facilitating Centre, Department of Science & Technology