A	B	C
1	Main
2		Brand Name	GS 9137, GS9350
3		Mechanism	integrase inhibitor, PK booster
4		Indication	HIV
5		Competition	MK-0518 in phase III; bid dosing showed 1.7-2.2log reduction at 10 days. P3 testing is for patients currently failing therapy
6		Admin	Oral qd
7		Marketing	QUAD pill to show less nightmares than Sustiva?
8		Safety	Lowers measured creatinine clearance. hOCT2 inhibition?
9		Clinical Trials
10			Phase III - begins in Q3/Q4 2007 - availability of MRK drug limits speed of this study
11			Likely non-inferiority study vs MRK drug.
12
13
14			Phase II - 2/23/07 - enrollment completed during Q206 - CROI 2007 - Zolopa et al.
15			n=278, 3-dose study in treatment-experienced patients
16			20mg, 50mgs and 125mgs qd boosted by 100mg of ritonavir; control is ritonavir-boosted PI regimen. Patients must have been on two prior antiretrovirals
17			Study met primary endpoint of non-inferiority vs protease inhibitors. P=0.02 for 125mg arm.
18			At 24 weeks GS9137 had -1.7 log reduction vs -1.2 log for boosted protease inhibitors
19			50mg had 38% undetectable at 16 weeks. 125mg had 40%. 64-84% of MK-518 was undetectable at 16 weeks in phase 2. Phase 3 data shows 60% vs 33-36% control.
20
21
22			Phase II treatment-naïve MK-0518+Truvada vs Sustiva+Truvada trial
23			2/8/2006: Integrase p1/2 data. 2-log reduction. Data presented at CROI.
24
25			Phase IIB treatment-naïve
26			n=198 randomized to Viread, Epivir and 100mg, 200mg, 400mg, 600mg MK-0518 bid or Sustiva qd
27			85-95% undetectable compared to 92% for Sustiva.
28			1 discontinuation due to elevated liver enzymes
29
30			Phase II treatment-experienced presented at ICAAC
31			24-weeks: 57-67% of MK-0518+SOC achieved HIV RNA <50copies/mL vs 14% of placebo+SOC.
32
33			p1/2 data evaluated the drug for 10 days as monotherapy
34			n=6 for each cohort; treatment-naïve and treatment experienced
35			200mg bid, 400mg bid, 800mg qd, 50mg qd (boosted with 100mg ritonavir), placebo
36			400mg and 800mg bid and 50mg+ritonavir had ~2.0 log reduction.