News

NEWS
For Immediate Release – October 24, 2007

Tranzyme Pharma’s Motilin Antagonist TZP-201 Shows Potential for
Preventing and Treating Chemotherapy-Induced Diarrhea (CID)
(Data to be Presented at the American Association for Cancer Research (AACR) Conference on Molecular Targets and Cancer Therapeutics) RESEARCH TRIANGLE PARK, N.C. and SHERBROOKE, Québec (October 24, 2007) -
Tranzyme Pharma, a leading biopharmaceutical company developing small molecule drugs for
the treatment of gastrointestinal and metabolic diseases, announced today that its Senior Vice
President of Research and Preclinical Development, Dr. Helmut Thomas, will present results of a
preclinical proof-of-concept study with its first-in-class motilin receptor antagonist TZP-201 at
the 2007 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer
Therapeutics
to be held in San Francisco, CA, on October 25, 2007.
Tranzyme is developing TZP-201, a highly potent and selective motilin antagonist, for the
treatment of gastrointestinal hypermotility disorders of various origins including chemotherapy-
induced diarrhea (CID). TZP-201 is the latest clinical candidate to emanate from Tranzyme
Pharma’s breakthrough small molecule macrocyclic (MATCH™) drug discovery technology.
In the presentation entitled “The Motilin Receptor Antagonist TZP-201 is Highly Effective in the
Control of Irinotecan Induced Diarrhea in Beagle Dogs”, Dr. Thomas will present data indicating
that TZP-201 can dose-dependently prevent or substantially mitigate otherwise lethal irinotecan-
induced diarrhea under conditions mimicking the clinical situation. In the study, TZP-201 was
shown to achieve its desired therapeutic results by reducing symptom severity and restoring
normal motility more effectively, more rapidly, and for a longer duration than the most common
current drug treatment options, loperamide and octreotide. The study also provided excellent
pharmacokinetic and safety data to support continued development of the compound.
“I am particularly excited that TZP-201 is not only highly effective in the control of established
CID, but even more so in the prevention of recurrence after repeated cycles of chemotherapy”
commented Dr. Thomas. “It may well be that we are on a pathway to prevent CID in a manner
equivalent to the ability of modern cancer support therapeutics to prevent chemotherapy-induced
nausea and vomiting. This property of the drug opens a new door to cytotoxic chemotherapy by
likely enabling an increase of dose and duration of treatment with improved chances of
completely eliminating malignancies at an earlier stage and preventing the appearance of
resistant tumor cells.”

About Chemotherapy Induced Diarrhea (CID)
Diarrhea is a common and serious side effect experienced by cancer patients as a result of the
detrimental effects of cytotoxic chemotherapy on the gastrointestinal tract. The incidence of CID
varies depending on the chemotherapeutic agent(s) used and drug dosing. In general, it is
estimated that 10% of patients with advanced cancer experience acute or persistent diarrhea that
may range from troublesome (grade 1) to lethal (grade 5) based on the National Cancer Institute-
Common Toxicity Criteria (NCI-CTC). Certain chemotherapy regimens, particularly those
including fluoropyrimidines (i.e., 5-FU), epothiolones and irinotecan, can result in diarrhea in
50% to 80% of patients, and more than 30% of patients may experience grade 3 to 5 diarrhea.
CID markedly impairs patient quality of life, creating increased anxiety, depression, discomfort,
and even travel limitations. At its extreme, diarrhea can also lead to life threatening
complications, including critical electrolyte imbalance, malnutrition, dehydration and
hemodynamic collapse. Importantly, CID can also negatively impact a patient’s treatment
outcome by necessitating dose reductions and interruptions in treatment, which consequently can
result in cancer disease progression or shorter survival.

About Tranzyme
Tranzyme Pharma is a biopharmaceutical company which discovers and develops breakthrough
small molecule drugs for diseases where there is a high unmet medical need. Tranzyme has
developed a pipeline of novel drugs for the treatment of gastrointestinal and metabolic diseases.
Tranzyme’s proprietary chemistry technology and discovery capabilities provide competitive
advantages in developing drugs being sought by pharmaceutical companies. For more
inform
CONTACTS
Vipin K. Garg, Ph.D.
Eric Nelson, Ph.D. VP, Business Development (919) 313-4759 [email protected]

Source: http://quakerbio.com/news/pcnews/2007/PR%20TZP-201%20Potential%20for%20CID%20FINAL%20102407.pdf

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