A	B	C	D	E	F	G	H	I	J	K
1	Main
2		Brand Name	Prezista, fka TMC114
3		Generic Name	darunavir
4		Mechanism	Protease inhibitor. Contains a 3R, 3a(S), 6aR-bis-tetrahydrofuranylurethane (bis-THF) group. Selected for its high 'genetic barrier' to resistance. Has a close fit within the substrate envelope.
5			Chemically similar to amprenavir (APV), but with substantially higher potency.
6		Administration	Oral
7		Indication	HIV
8		IP	2012 to 2015.
9		Efficacy	-1.7 to -2.0 logs vs -0.63 in POWER1
10		Side Effects	Mostly benign. Diarrhea, nausea, headache.
11		Timeline	June 23rd 2006 PDUFA. Filed in late 2005.
12		Notes	Kaletra has 1.1B run-rate. better resistance profile? Aimed for 2L. Might be able to file with phase 2?
13		Clinical Studies
14			TMC114-C226: EAP
15			TMC114-C211: TMC114 vs Kaletra in tx-naïve pts. N=660. Study start 9/2005. Still enrolling as of 5/2006.
16			ARTEMIS? 84% <50copies vs 78% undectectable.
17			TMC114-C207: p2a POC study presented at Feb 2003 Boston CROI
18			TMC114-C202:POWER2: ongoing for 144 weeks. Data presented at ICAAC 2005.
19				n=278 who have failed 3 therapies. 62% of patients achieved 1log or more vs 14% for control group. 39% undetectable vs 7% for control arm.
20			TMC114-C213:POWER1: ongoing for 144 weeks. 24wk data presented at IAS 2005.
21				Presentations		1	2	3
22			TMC114-C214: pivotal p3 study in moderately tx-experienced patients
23						3	4	5
24
25
26			2006	2007	2008	2009	2010	2011	2012	2013	2014
27		TMC114	30	248.2	413.25	565.5	672.75	746.79	834.0285	905.8856850000001	960.95633355
28		Bear Estimate	25	181	413	611	781
29
30			2000	2001	2002	2003	2004	2005	2006	2007	2008
31		Kaletra	30	292	551	754	897	995.72	1112.038	1207.84758	1281.2751114