Asco Abstracts

Up!

UCB’s got a chart

go check it out.

TG-101348

Targegen’s got a press release:

Plans to initiate a multi-center clinical trial of TG101348, an internally discovered, oral, potent, and highly selective JAK2 inhibitor in January, 2008

A poster at ASH:

…Dual-Acting JAK2/FLT3 Small Molecule Kinase Inhibitor for the Treatment of AML

and some pyrimidines in WO/2007/053452:

AACR NCI EORTC

Abstracts are up, and B is the one you’ll be looking for.

News of the day:

In pts [patients] with PRC, XL-880 demonstrated antitumor activity

Name	Target	Company	Phase
AZD-2171	Vegf c-Kit Pdgfr-β	AstraZeneca	ph2
AZD-2171	Vegf c-Kit Pdgfr-β	AstraZeneca	ph2
PD-325901	Mek	Pfizer	ph2
XL-647	ErbB1,2 Vegfr-2	Exelixis	ph2
XL-880	c-Met Vegf	Exelixis	ph2
ARQ-197	c-Met	Arqule	ph1
BAY-579352	Vegfr-2,3 c-Kit Pdgfr-β	Bayer	ph1
BAY-734506	c-Kit Ret Pdgfr Raf	Bayer	ph1
BIBW-2992	ErbB (irrev)	BI	ph1
PD-325901	Mek	Pfizer	ph1
PF-299804	ErbB (irrev)	Pfizer	ph1
Ticribine	Akt	VioQuest	ph1
XL-647	ErbB 1,2 Vegfr-2	Exelixis	ph1
XL-820	Vegfr c-Kit Pdgfr	Exelixis	ph1
XL-880	c-Met Vegf	Exelixis	ph1
ARRY-543	ErbB1, 2	Array	ph1
AT-13148	Akt Rock PKA	Astex
AV-951	Vegf	Aveo	ph1
BAY-734506	c-Kit Ret Pdgfr Raf	Bayer
BMS-698769	c-Met	BMS
CEP-11981	Tie2 Vegfr	Cephalon
CUDC-101	HDAC / ErbB	Curis
NVP-BEZ235	Pi3k	Novartis
OSI-906	IGF-1R	Osi
RDEA-119	Mek	Ardea
SGX-523	c-Met	SGX
SR-13654	Src	SRI
XL-765	Pi3k, mTOR	Exelixis
XL-820	c-Kit	Exelixis
XL-844	Chk1, 2	Exelixis
ZD-6474	Vegfr-2 EGFR
ZM 447439	Aurora
CRT-59359	PKD	CRT

Duplicates and phase field just reflect the subject of the poster / reported trial, click for more details.

Steal This Document

You may have noticed the Ro5 tab above. Here’s the spreadsheet.

To the best of my knowledge it’s the most complete list of clinical stage kinase inhibitors in existence. There are bound to be errors and omissions though, so while I of course don’t want anything proprietary please send me references and structures as appropriate. I appreciate the help.

Clinical Roundup

Pharmacopoeia - earned a milestone for p38 inhibitor BMS-582949 going ph2.

Incyte – reported on ph2 Jak inhibitor INCB-18424 (?WO/2005/105814, 2B7A) (decent webcast here The short of it: pretty much the same as steroids … no adverse effects at any dose. check in ~8 minutes).

Exelixis – will bundle reports for ph2 XL-880, XL-647, and ph1 XL-184, XL820, and XL-147 at AACR later this month. The Fools think GSK will pick up 880 and I tend to agree.

Ambit talked about a lot at UBS and updates on AC-220 (ph1 FLT3 inhibitor).

Ardea (RDEA)- is preparing to list on the Nasdaq and has RDEA-119 about to hit ph1.

SGX – spins a yarn suggesting that Novartis took a pass on SGX-393. IND for a different compound expected mid ’08. (Webcast on Thursday)

Ariad – knows all about T315I and SGX… Still no structure for AP-24534 though… IND expected end of the year.

S*Bio – has SB-1518 an oral Jak2 (V617F) inhibitor in development: WO/2007/058628, WO/2007/058627

clinical roundup

Supergen initiates dosing of flt3 inhibitor MP-470: ph1 ‘advanced-stage solid tumors.’

Entremed initiates trial for Aurora inihbitor MKC-1: Ph1 Leukemia

Kinex gets the FDA go-ahead for Src inhibitor KX2-391: lymphoma or solid tumors (though despite the press release, it’s not the first non-atp competitive kinase inhibitor to enter the clinic. The MEK inhibitors were)

R763

Rigel’s Aurora inhibitor R-763 going Ph1 for ‘Hematological Malignancies’. It’s in Ph1 for solid tumors already. hmm… I thought they had to call it ‘EMD Serono’ in USA.  Merck DE # is: AS703569

So it’s looking like: WO/2006/055561 and before that: WO/2005/118544

Neeto – looks like they resolve the enantiomers via:

Even neeter-0 they show a couple xenos

INNO-406

Making some bold claims, Innovive gets orphan status for INNO-406 / NS-187

…speechless

XL518

Exelixis is on fire these days. 518′s IND is in the books.