Tesaro Summarizes Phase 3 Rolapitant Data Presented at the 2014 American Society of Clinical Oncology (ASCO) Annual Meeting and

Tesaro Summarizes Phase 3 Rolapitant Data Presented at the 2014 American
Society of Clinical Oncology (ASCO) Annual Meeting and Provides an Update on
Niraparib Development Strategy

  *Oral Rolapitant New Drug Application (NDA) Submission on Track for
    Mid-2014
  *Development Plans for Niraparib in Small Cell Lung Cancer and First-Line
    Ovarian Cancer Announced

CHICAGO, June 1, 2014 (GLOBE NEWSWIRE) -- TESARO, Inc. (Nasdaq:TSRO), an
oncology-focused biopharmaceutical company, today announced that final results
from three Phase 3 trials of rolapitant, an investigational neurokinin-1
(NK-1) receptor antagonist in development for the prevention of
chemotherapy-induced nausea and vomiting (CINV), were presented today at the
American Society of Clinical Oncology (ASCO) annual meeting in Chicago.

"We are very pleased with these pivotal data which, along with the previously
conducted Phase 2 study, will form the basis of our New Drug Application
submission to the U.S. Food and Drug Administration in mid-2014," said Mary
Lynne Hedley, Ph.D., president of TESARO. "Additionally, we look forward to
expanding our niraparib development program to include clinical trials in the
small cell lung cancer and first line ovarian cancer settings."

Phase 3 Results

The first Phase 3 study of rolapitant was an international, multicenter,
randomized, double-blind, active-controlled study that enrolled 1,369 cancer
patients receiving moderately emetogenic chemotherapy (MEC), approximately
half of whom were receiving anthracycline-based treatment for breast cancer.
Patients were randomized to receive either control, which consisted of a
5-HT[3] receptor antagonist plus dexamethasone, or 200 milligrams of oral
rolapitant plus control. Patients who received rolapitant had a significantly
higher complete response (CR) rate, defined as no emesis and no use of rescue
medication, for the primary endpoint of complete response during the delayed
phase compared to control (71.3% vs. 61.6%, p<0.001). CR rates were higher for
rolapitant-treated patients in the acute (83.5% vs 80.3%, p=0.143) and overall
(68.6% vs. 57.8%, p<0.001) phases. The rolapitant group also achieved higher
rates of complete protection, defined as no emesis, no use of rescue
medication, and no significant nausea, in both the delayed (64.3% vs. 56.9%,
p=0.006) and overall phases (62.0% vs. 53.2%, p=0.001). Approximately
one-third of the participants (n=457/1,369) in this trial were enrolled at
U.S.-based clinical sites, and a subset analysis of these patients showed that
the rolapitant group had higher CR rates in the delayed (61.6% vs. 48.0%,
p=0.005), acute (84.7% vs. 75.1%; p=0.012) and overall (59.3% vs. 44.1%,
p=0.002) phases, in addition to higher rates of complete protection overall
(54.2% vs. 39.7%, p=0.042), no significant nausea overall (68.1% vs. 58.5%,
p=0.003), and no emesis overall (78.7% vs. 65.3%, p>0.001).

The second Phase 3 study of rolapitant was an international, multicenter,
randomized, double-blind, active-controlled study that enrolled 532 patients
receiving highly emetogenic chemotherapy (HEC), defined as regimens which
contain cisplatin at a dose equal to or greater than 60 mg/m^2. Patients were
randomized to receive either control, which consisted of a 5-HT[3] receptor
antagonist plus dexamethasone, or 200 milligrams of oral rolapitant plus
control. Patients who received rolapitant had a significantly higher complete
response rate compared to control for the primary endpoint of CR during the
delayed phase (72.7% vs. 58.4%, p<0.001), acute (83.7% vs 73.7%, p=0.005) and
overall (70.1% vs. 56.5%, p=0.001) phases. Additionally, rolapitant-treated
patients had a significantly higher rate of no significant nausea in the
overall phase (71.6% vs. 63.0%, p=0.037). The rolapitant group also achieved
higher rates of no nausea in both the delayed (53.0% vs. 41.6%, p=0.009) and
overall phases (49.6% vs. 39.3%, p=0.018).

The third Phase 3 study of rolapitant was an international, multicenter,
randomized, double-blind, active-controlled study that enrolled 555 patients
receiving highly emetogenic chemotherapy (HEC), defined as regimens which
contain cisplatin at a dose equal to or greater than 60 mg/m^2. Patients were
randomized to receive either control, which consisted of 5-HT[3] receptor
antagonist plus dexamethasone, or 200 milligrams of oral rolapitant plus
control. Patients who received rolapitant had a significantly higher complete
response rate compared to control for the primary endpoint of CR during the
delayed phase (70.1% vs. 61.9%, p=0.043). CR rates were also higher for
rolapitant-treated patients in the acute (83.4% vs 79.5%, p=0.233) and overall
(67.5% vs. 60.4%, p=0.084) phases. The rolapitant group also achieved higher
rates of no nausea in both the delayed (58.3% vs. 46.9%, p=0.007) and overall
phases (55.0% vs. 44.0%, p=0.009).

Safety & Tolerability Data

Safety and tolerability data for patients who received rolapitant were similar
to the results for those who received control in each of the three Phase 3
trials, and were consistent with the results from earlier rolapitant clinical
studies. The most frequently reported treatment-related adverse events were
balanced across treatment arms and included fatigue, constipation, headache,
nausea, hiccups and dyspepsia.

Preparations continue in support of a submission of a New Drug Application
(NDA) to the U.S. Food and Drug Administration (FDA) in mid-2014. The oral
rolapitant NDA will include data from one Phase 3 study in patients receiving
moderately emetogenic chemotherapy (MEC), in addition to one Phase 2 and two
Phase 3 trials in patients receiving cisplatin-based, highly emetogenic
chemotherapy (HEC). The top-line results of each of the Phase 3 trials of
rolapitant were previously announced by TESARO.

Rolapitant is an investigational agent and, as such, has not been approved by
the U.S. FDA or any other regulatory agency. The p values presented above are
unadjusted.

About Rolapitant

Rolapitant is a potent and selective NK-1 receptor antagonist with an extended
plasma half-life that is being developed for the prevention of CINV. NK-1
receptors are highly concentrated in the brain and bind the neurokinin
substance P. Activation of NK-1 receptors plays a central role in nausea and
vomiting induced by emetogenic stimuli, including certain cancer
chemotherapies. NK-1 receptor antagonists have been demonstrated to improve
the management of nausea and vomiting experienced by cancer patients
undergoing chemotherapy. The safety and tolerability of single and repeat
doses of rolapitant have been assessed in more than 2,500 healthy volunteers
and patients. Rolapitant is being developed both in oral and intravenous
formulations. TESARO licensed exclusive rights for the development,
manufacture, commercialization and distribution of rolapitant from OPKO
Health, Inc.

About Chemotherapy-Induced Nausea and Vomiting (CINV)

CINV is estimated to afflict over 70% of cancer patients undergoing
chemotherapy and, if not prevented, may possibly result in a delay or even
discontinuation of chemotherapy treatment.Prolonged nausea and vomiting may
result in unwanted weight loss, dehydration and malnutrition, as well as
hospitalization.

About TESARO

TESARO is an oncology-focused biopharmaceutical company dedicated to improving
the lives of cancer patients by acquiring, developing and commercializing
safer and more effective therapeutics. For more information, visit
www.tesarobio.com.

To the extent that statements contained in this press release are not
descriptions of historical facts regarding TESARO, they are forward-looking
statements reflecting the current beliefs and expectations of management made
pursuant to the safe harbor provisions of the Private Securities Litigation
Reform Act of 1995. Words such as "may," "will," "expect," "anticipate,"
"estimate," "intend," and similar expressions (as well as other words or
expressions referencing future events, conditions or circumstances) are
intended to identify forward-looking statements.Examples of forward looking
statements contained in this press release include our expectations regarding
future clinical trials with niraparib. Forward-looking statements in this
release involve substantial risks and uncertainties that could cause our
clinical development programs, future results, performance or achievements to
differ significantly from those expressed or implied by the forward-looking
statements. Such risks and uncertainties include, among others, the
uncertainties inherent in the initiation of future clinical trials,
availability of data from ongoing clinical trials, expectations for regulatory
approvals, and other matters that could affect the availability or commercial
potential of our drug candidates. TESARO undertakes no obligation to update or
revise any forward-looking statements. For a further description of the risks
and uncertainties that could cause actual results to differ from those
expressed in these forward-looking statements, as well as risks relating to
the business of the Company in general, see TESARO's Annual Report on Form
10-K for the year ended December 31, 2013 and other filings TESARO makes with
the Securities and Exchange Commission.

CONTACT: Investor/Media Contact:
         Jennifer Davis
         Sr. Director, Corporate Development & Investor Relations
         +1.781.325.1116 or jdavis@tesarobio.com

TESARO, Inc. Logo
 
Press spacebar to pause and continue. Press esc to stop.