A	B	C	D	E
1	Main
2		Brand Name	Januvia, Janumet, MK-0431/A
3		Generic Name	sitagliptin
4		Indication	Type 2 diabetes mellitus.
5		Mechanism	DPP4 inhibitor. Dipeptidyl peptidase-4 inhibition potentiates endogenous peptides known as incretins.
6			Native GLP1 effectively lowers blood glucose but is rapidly degraded by DPP4. Byetta is DPP4-resistant.
7			DPP4 is a membrane-spanning cell-anchored protein expressed on many cell types. It also has a soluble form in circulation.
8		Price	$4.86 a day
9		Dosing	qd dosing vs bid dosing for Galvus
10			planning fixed combination with metformin. That will be filed in 2007 but will be twice daily
11		Papers	Fresh from the pipeline: sitagliptin. Drucker et al. Nature Reviews Drug Discovery, Volume 6, Feb 2007. 109.
12			The biology of incretin mhormones. Cell Metab. 3,153-165(2006). Drucker, D.
13			Therapeutic strategies based on glucagon-like peptide-1. Diabetes 53,2181-2189(2004). Deacon et al.
14			Enhanced insulin secretion and improved glucose tolerance in mice lacking CD26. PNAS 97,6874-6879(2000). Marguet et al.
15		History	Approved October 2006.
16		IP	2017-2026.
17			2026, 7326708: salt patent.
18			2022, 6699871: COM patent issued 3/2/2004. Filed 7/5/2002.
19			2017, 6303661: DPP4 method patent.
20		Clinical Trials
21			ADA Abstracts
22				556-P	24-week data showed PBO-subtracted 0.70% a1c decrease; (8% baseline)
23				1995-PO	24-week data showed PBO-subtracted 0.79% and 0.94% a1c decrease (8% baseline)
24				1996-PO	24-week data showed PBO-subtracted 0.60% and 0.48% a1c decrease (8.1% baseline)
25
26			ACT NOW - ADA 2008
27			supports earlier use of glucose control to delay onset of diabetes
28
29		Rx
30				NRX	TRX
31			11/14/2008
32			11/7/2008	70921	198960
33			10/31/2008
34			10/24/2008
35			10/17/2008
36			10/5/2007	37141	94650
37			9/28/2007	36584	89911
38			9/21/2007	36273	88447
39			9/14/2007
40			9/7/2007
41			8/31/2007
42			8/24/2007
43			8/17/2007
44			8/10/2007
45			8/3/2007
46			7/27/2007
47			7/20/2007
48			7/13/2007
49			7/6/2007
50			6/29/2007
51			6/22/2007
52			6/15/2007
53			6/8/2007
54			6/1/2007
55			5/25/2007
56			5/18/2007
57			5/11/2007
58			5/4/2007
59			4/27/2007
60			4/20/2007	21590	43676
61			4/13/2007	20981	42146
62			4/6/2007	21119	41949
63			3/30/2007
64			3/23/2007
65			3/16/2007
66			3/9/2007
67			3/2/2007
68			2/23/2007
69			2/16/2007
70			2/9/2007
71			2/2/2007
72			1/26/2007
73			1/19/2007
74			1/12/2007	16007	22641
75			1/5/2007	12984	18705
76			12/29/2006	11492	15624
77			12/22/2006	13343	16352
78			12/15/2006	12660	15185
79			12/8/2006		13285
80			12/1/2006		10771
81			11/24/2006		6765
82			11/17/2006		7231