Leap Therapeutics Presents Data from Phase 1 Single Dose Safety Study of Anti-GITR Immunotherapy TRX518 in Patients with Advanced Relapsed or Refractory Solid Tumors at American Society of Clinical Oncology (ASCO) 2016 Annual Meeting

On June 5, 2016 Leap Therapeutics, a company developing immuno-oncology therapeutics, reported results of a Phase 1 clinical trial of TRX518, an aglycosylated monoclonal agonist antibody targeting glucocorticoid-induced TNFR-related (GITR) protein (Press release, Leap Therapeutics, JUN 5, 2016, View Source [SID:1234513091]). The Phase 1 trial demonstrated that a single dose of TRX518 in patients with advanced solid tumors was safe and well-tolerated. There were no autoimmune treatment-related adverse events. Saturation of TRX518 on GITR on T cells in peripheral blood was observed, and exposures demonstrating efficacy in preclinical models were safely reached. Henry Koon, M.D., of the University Hospitals, presented the data at the 2016 Annual Meeting of the American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper).

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"The safety and pharmacokinetic results from this clinical study have allowed us to further develop the drug in a repeat-dose study. We look forward to the exploring the activity of TRX518 as a single-agent and in combinations," commented Dr. Koon.

Leap is enrolling patients in two clinical studies in patients with advanced solid tumors to assess the safety, pharmacokinetics, pharmacodynamics, and efficacy of TRX518 when dosed at various dose levels and frequencies.

"GITR is emerging as an important target in regulating anti-tumor immune responses. Preclinical studies have shown that agonist anti-GITR antibodies can modulate inhibitory and stimulatory signals, which may potentiate anti-cancer immune responses," commented Jedd Wolchok, M.D., Ph.D., Chief of Melanoma and Immunotherapeutics Service at Memorial Sloan Kettering Cancer Center and the principal investigator in Leap’s TRX518 study.

About TRX518

TRX518 is a humanized aglycosyl IgG1 monoclonal antibody with agonist activity targeting GITR. TRX518 has been shown to bind and activate GITR through bivalent binding to the receptor. TRX518 was engineered to remove Fc-receptor interactions to prevent complement-mediated cytolysis and antibody-mediated depletion of leukocytes expressing GITR. TRX518 surrogate antibodies have been effective in preclinical animal models, prolonging survival or enhancing immune responses when combined with chemotherapeutics and checkpoint inhibitors.

Exelixis Announces Genentech Presentation of Preliminary Phase 1B Trial Results for the Combination of Cobimetinib and Atezolizumab at ASCO 2016 Annual Meeting

On June 5, 2016 Exelixis, Inc. (NASDAQ:EXEL) reported that its collaborator Genentech, a member of the Roche Group, will present preliminary results from a phase 1b clinical trial evaluating the safety and clinical activity of cobimetinib, an Exelixis-discovered MEK inhibitor, in combination with atezolizumab, an anti-PD-L1 antibody discovered and developed by Genentech, in patients with metastatic colorectal cancer (CRC) (Press release, Exelixis, JUN 5, 2016, View Source;p=RssLanding&cat=news&id=2175111 [SID:1234513003]). The results will be the subject of an oral presentation (Abstract #3502) today at the 2016 American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting, which is being held June 3-7 in Chicago, Illinois. Johanna Bendell, M.D., director of the Gastrointestinal Cancer Research Program at the Sarah Cannon Research Institute/Tennessee Oncology, Nashville, Tennessee, will present the results.

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"These early data on the combination of cobimetinib, an Exelixis-discovered MEK inhibitor, and atezolizumab, an anti-PD-L1 antibody discovered and developed by Genentech, are encouraging and warrant further study in people with previously-treated metastatic colorectal cancer, including those with microsatellite stable disease," said Michael M. Morrissey, Ph.D., president and chief executive officer of Exelixis. "Based on these results, Genentech has initiated the COTEZO phase 3 trial in patients with unresectable locally advanced or metastatic colorectal cancer."

This ongoing phase 1b trial includes both a dose escalation stage and dose expansion stage. The trial’s primary objective is the evaluation of the safety and tolerability of the combination. Secondary endpoints include objective response rate (ORR) per RECIST, duration of response, progression-free survival (PFS), overall survival (OS), as well as evaluation of biomarkers.

As of the February 12, 2016 data cut-off, 23 patients with advanced CRC (22 with mutant KRAS and one with wild-type KRAS) were enrolled during the trial’s escalation and expansion phases. No dose-limiting toxicities were observed. The median follow-up for safety in CRC patients was 3.8 months, with a range of 1.1 to 15.1 months. There were no all-cause grade 5 or treatment-related grade 4 AEs reported, and incidence of treatment-related grade 3 AEs was 35% (n=8). The most common treatment-related AEs, regardless of severity, included: diarrhea (70% of patients); fatigue (52%); dermatitis acneiform (44%); rash (35%); and nausea, maculopapular rash and pruritus (each 26%).

The ORR for the combination was 17%, including four confirmed partial responses; additionally five patients achieved stable disease. The median duration of response was not yet reached, with a range of 5.4 to more than 11.1 months.

Median PFS for all CRC patients enrolled in the trial was 2.3 months, with a range of 1.8 to 9.5 months. The six-month PFS was 35%. Median OS for all CRC patients was not evaluable, while six-month OS was 72%.

Recently Initiated COTEZO Phase 3 Pivotal Trial

In June 2016 Genentech initiated COTEZO, a phase 3 pivotal trial of the combination of cobimetinib and atezolizumab in unresectable locally advanced or metastatic colorectal cancer. The trial is expected to enroll 360 patients who have received at least two prior chemotherapies in the metastatic disease setting. The primary endpoint of the COTEZO trial is overall survival. More information about the COTEZO phase 3 pivotal trial is available at www.clinicaltrials.gov.

Additional Cobimetinib Data Presented at ASCO (Free ASCO Whitepaper) 2016

The oral presentation in colorectal cancer is one of eight cobimetinib abstracts being presented at the ASCO (Free ASCO Whitepaper) 2016 Annual Meeting this week. Additional data presentations include studies of cobimetinib in combination with other therapies to treat triple-negative breast cancer and BRAF-mutant melanoma. For full logistical information on these other presentations, please see Exelixis’ ASCO (Free ASCO Whitepaper) announcement press release issued on April 20, 2016, available online here.

About the Cobimetinib Development Collaboration

Exelixis discovered cobimetinib internally and advanced the compound to investigational new drug (IND) status. In late 2006, Exelixis entered into a worldwide collaboration agreement with Genentech, under which Exelixis received initial upfront and milestone payments for signing the agreement and submitting the IND. Following the determination of the maximum tolerated dose in phase 1 by Exelixis, Genentech exercised its option to further develop cobimetinib.

Under the terms of the collaboration, Exelixis is entitled to an initial equal share of U.S. profits and losses resulting from sales of cobimetinib to treat any form of cancer, which will decrease as sales increase, and will share in U.S. marketing and commercialization costs. In November 2013, Exelixis exercised its option to co-promote cobimetinib in the United States and, under the terms of the agreement, the company is fielding 25 percent of the U.S. sales force for the product’s first commercial indication in specific forms of BRAF mutation-positive advanced melanoma, closely coordinating its efforts with Genentech. Outside of the United States, Exelixis is eligible to receive royalties on any sales.

Cobimetinib in combination with vemurafenib is now approved in multiple countries, including the United States, European Union, Switzerland, Canada, Australia and Brazil, to treat specific forms of BRAF mutation-positive advanced melanoma. Further country approvals are anticipated in 2016 and beyond. Cobimetinib is also the subject of a clinical development program aimed at evaluating its potential in combination with a variety of investigational and approved therapies in disease settings including metastatic melanoma, triple-negative breast cancer and advanced solid tumors.

COTELLIC Indication

COTELLIC (cobimetinib) is a prescription medicine that is used with ZELBORAF (vemurafenib), to treat a type of skin cancer called melanoma that has spread to other parts of the body or cannot be removed by surgery, and that has a certain type of abnormal "BRAF" gene.

A patient’s healthcare provider will perform a test for the BRAF gene to make sure that COTELLIC is right for them. It is not known if COTELLIC is safe and effective in children under 18 years of age.

COTELLIC Important Safety Information

Patients should avoid sunlight during treatment with COTELLIC. COTELLIC can make their skin sensitive to sunlight. They may burn more easily and get severe sunburns. To help protect against sunburn, they should wear clothes that protect their skin, including their head, face, hands, arms, and legs. They should use lip balm and a broad-spectrum sunscreen with SPF 30 or higher.

COTELLIC may cause serious side effects, including risk of new skin cancers, bleeding problems, heart problems, severe rash, eye problems, liver problems, muscle problems (rhabdomyolysis), and photosensitivity. Patients should tell their doctor if they are pregnant or plan to become pregnant, as COTELLIC and ZELBORAF can harm an unborn baby. Patients who take COTELLIC should use effective methods of birth control during treatment, for 2 weeks after stopping COTELLIC, and for at least 2 months after stopping ZELBORAF. Do not breastfeed during treatment with COTELLIC and for 2 weeks after the final dose. Patients along with their healthcare provider should decide if they will take ZELBORAF or breastfeed. Patients should not do both.

Patients should tell their healthcare provider about all the medicines they take. Some types of medicines will affect the blood levels of COTELLIC.

Common side effects of COTELLIC include diarrhea, sunburn or sun sensitivity, nausea, fever, and vomiting. COTELLIC can also cause changes in blood test results.

Patients should tell their healthcare provider if they have any side effect that bothers them or that does not go away. These are not all the possible side effects of COTELLIC. For more information about side effects, patients should ask their healthcare provider or pharmacist.

Patients should call their doctor for medical advice about side effects. They may report side effects to FDA at (800) FDA-1088 or www.fda.gov/medwatch. They may also report side effects to Genentech at (888) 835-2555.

Please see full COTELLIC Prescribing Information and Patient Information for additional Important Safety Information.

Xcovery Presents Results of Plasma Genotyping of Patients in the eXalt2 Study at the ASCO Annual Meeting 2016

On June 5, 2016 Xcovery, a developer of targeted therapeutics for cancer, reported that results from an expansion cohort in the ongoing Phase I/II clinical study of its investigational tyrosine kinase inhibitor (TKI), ensartinib (X-396), in patients with anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer (NSCLC) were presented at the American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting 2016 held in Chicago, Illinois (Press release, Xcovery, JUN 5, 2016, View Source [SID:1234513092]).

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Results from this multicenter expansion study demonstrated that ensartinib is well-tolerated and induces response in both crizotinib-naive and crizotinib-resistant ALK-positive NSCLC patients, as well as patients with CNS disease. The results also showed that plasma NGS with the Resolution ctDxTM blood-based platform may be used to detect ALK kinase domain mutations to select patients for therapy and monitor changes in response to treatment in a non-invasive manner. Results were presented by Dr. Leora Horn, MD, MSc, Vanderbilt University Medical Center, in a poster titled "Plasma genotyping of patients in the eXalt2 trial: ensartinib+ (X-396) in ALK-positive non-small cell lung cancer (NSCLC)."

"Ensartinib has shown promising activity in ALK-positive NSCLC patients with durable responses observed in patients who are crizotinib-naïve and patients with resistance to crizotinib and second generation ALK tyrosine kinase inhibitors," said Dr. Horn. "The plasma sequencing of patients in the expansion study have identified a potential way to identify and select patients for therapy and to monitor for response and the development of acquired resistance."

About the Expansion Cohort of the Phase I/II "eXalt2" Study

In this multicenter study, 38 patients with ALK-positive (via FISH or IHC) advanced or recurrent NSCLC were treated with at least 200mg of ensartinib on 28-day cycles with plasma samples collected on the first day of each cycle. Major inclusion criteria for the expansion cohort included: ALK-positive (via FISH or IHC) advanced or recurrent NSCLC, measurable disease and ECOG performance status (PS) 0-1. Asymptomatic treated or untreated brain metastases (CNS) and leptomeningeal disease were allowed.

Key conclusions from the study include:

Ensartinib has shown promising activity in ALK-positive NSCLC patients with durable responses observed in patients who are crizotinib-naïve and patients with resistance to crizotinib and second generation ALK TKIs.
Plasma NGS can be used to detect ALK kinase domain mutations and monitor changes in response to treatment in a non-invasive manner.
In this study, ALK kinase domain mutations were detected in 4/11 patients who had prior crizotinib and 2/4 patients who had prior crizotinib and ceritinib. G1202R was found in both of the latter cases.
1/2 patients whose plasma detected the G1202R mutation prior to start of the trial responded to ensartinib.
Further study of this methodology is ongoing to correlate the presence of ALK kinase domain mutations with response and resistance to ALK TKI therapy.
A Phase III trial is ongoing comparing ensartinib to crizotinib in TKI naïve ALK-positive NSCLC patients.
About Ensartinib (X-396)

Xcovery’s lead asset is X-396, a small molecule, anaplastic lymphoma kinase (ALK) inhibitor. It is being studied in the Xalt2 Study, a phase II trial for the treatment of ALK-positive non-small cell lung cancer (NSCLC). The Xalt2 Study is currently enrolling patients. To learn more, visit: www.xalt2study.com or ClinicalTrials.gov under trial identifier NCT01625234.

About NSCLC and ALK

Lung cancer is the second most common type of cancer identified in the United States with an estimated 221,000 new diagnoses expected in 2015. Non-small cell lung cancer (NSCLC) is the most common type of lung cancer, accounting for an estimated 85-90% of the lung cancer cases. The anaplastic lymphoma kinase (ALK) gene is located on chromosome 2 and rearrangement of the ALK gene can lead to its activation or expression, therefore increasing a person’s chance of developing certain types of cancer, including NSCLC. Between three and seven percent of patients with NSCLC have the ALK rearrangement, making this a molecular target warranting investigation for NSCLC patients.

[PDF]Kyowa Hakko Kirin Announces Preliminary Results from Pivotal Phase 2 Study of Mogamulizumab (KW-0761) in Patients with Relapsed or Refractory Adult T-cell Leukemia-Lymphoma

On June 6, 2016 Kyowa Hakko Kirin Co., Ltd. (Tokyo; 4151 President and CEO: Nobuo Hanai; "Kyowa Hakko Kirin") reported the preliminary results today from the pivotal Phase 2 study of mogamulizumab (Code name: KW-0761) for the treatment of Adult T-cell Leukemia-Lymphoma (ATL) (Press release, Kyowa Hakko Kirin, JUN 5, 2016, View Source [SID:1234513141]).

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"We are very pleased to announce that we have completed the largest, prospective randomized clinical trial for relapsed/refractory ATL and that the preliminary results of this pivotal Phase 2 study showed potential of mogamulizumab for the treatment of relapsed/refractory ATL, where no standard of care exists" said Yoichi Sato, Managing Executive Officer, Vice President, Head of Research and Development Division of Kyowa Hakko Kirin.

Study Design
Patients from the USA, EU, and Latin America with aggressive relapsed or refractory ATL were randomized 2:1 to treatment with mogamulizumab or to 1 of 3 investigator choice (IC) regimens (Gem/Ox, DHAP or pralatrexate). Patients in the IC arm were permitted to cross-over to treatment with mogamulizumab after progression. Overall Response Rate (ORR; confirmed and unconfirmed) was assessed by the treating investigator (IA) and through blinded assessment by independent review (IR).

Study Results
71 patients were randomized (47 to mogamulizumab, 24 to IC). In the mogamulizumab treated group, unconfirmed ORR was 28% (13/47) by IR and 34% (16/47) by IA, while in the IC group, unconfirmed ORR was 8% (2/24) by IR and 0/24 by IA. Confirmed ORR (response maintained at successive evaluations approximately 8 weeks apart) for mogamulizumab was 11% by IR and 15% by IA, while there were no confirmed responses in the IC group. 18 out of 24 patients in the IC arm crossed over to mogamulizumab and 3 patients (17%) responded (1 of the responses was confirmed). The median duration of confirmed response for mogamulizumab was 5.0 months by IR and 5.5 months by IA. One patient had a response lasting more than 9 months. The frequently observed treatment-emergent, adverse events in the mogamulizumab arm included infusion reactions (46.8%), rash/drug eruption (19.1%) and infections (51.1%). The safety data collected from this study were similar to what has previously been documented.

These data from the study were presented at the American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting on June 5th, 2016.
The Kyowa Hakko Kirin Group companies strive to contribute to the health and well-being of people around the world by creating new value through the pursuit of advances in life sciences and technologies.

About Mogamulizumab
Mogamulizumab is a humanized mAb directed against CC chemokine receptor 4 (CCR4), which is frequently expressed on leukemic cells of certain hematologic malignancies including ATL. Mogamulizumab was produced using Kyowa Hakko Kirin’s proprietary POTELLIGENT platform, which is associated with enhanced antibody-dependent cellular cytotoxicity (ADCC), and was launched in Japan in May 2012 for the treatment of patients with relapsed or refractory CCR4-positive ATL under the trade name POTELIGEO. The drug was approved for indication expansion and was granted marketing authorization in Japan for the treatment of patients with relapsed or refractory CCR4-positive, peripheral T-cell lymphoma (PTCL) and cutaneous T-cell lymphoma (CTCL) in March 2014, and with chemotherapy-naive CCR4-positive ATL in December 2014.

About Adult T-cell Leukemia-Lymphoma (ATL)
ATL is a disease entity within the category of mature T- and NK-cell neoplasms, according to the classification by the World Health Organization. It is an extremely aggressive T lymphocytic malignancy that originates in T-cells infected with the human T-lymphotropic virus-1(HTLV-1). ATL has a very distinct epidemiology and geographic distribution, primarily involving areas of Japan, the Caribbean Basin, parts of South America, the Middle East and sub-Saharan Africa, where HTLV-1 infection is endemic. In non-endemic regions such as North America and Europe, HTLV-1 infection is mainly found in immigrants from endemic areas, their offspring or sexual contacts. Treatment regimens for ATL have not been standardized, especially in the relapsed/refractory setting, representing a large unmet medical need in this patient population.

Exelixis and Its Partner Ipsen Announce Phase 3 Trial Results of CABOMETYX™ (Cabozantinib) Tablets Demonstrating Significant Overall Survival Benefit for Previously Treated Patients with Advanced Renal Cell Carcinoma Presented at ASCO

On June 5, 2016 Exelixis, Inc. (NASDAQ:EXEL) and Ipsen (Euronext:IPN; ADR:IPSEY) reported overall survival (OS) results from the phase 3 METEOR trial of CABOMETYX (cabozantinib) tablets in patients with advanced renal cell carcinoma (RCC) who have received prior anti-angiogenic therapy (Press release, Exelixis, JUN 5, 2016, View Source;p=RssLanding&cat=news&id=2175112 [SID:1234513004]). The findings will be presented during an oral abstract session today at the 2016 American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting in Chicago, and were published today in The Lancet Oncology.1 The OS results demonstrate that CABOMETYX reduces the risk of death by one third versus everolimus.

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Exelixis previously announced that METEOR met its primary endpoint, progression-free survival (PFS), and secondary endpoints, OS and objective response rate.

"The overall survival benefit conferred by treatment with CABOMETYX — which was consistently favorable across a variety of prespecified and post-hoc patient subgroups — is a strong complement to the progression-free survival and objective response rate findings previously reported," said Toni Choueiri, M.D., Clinical Director, Lank Center for Genitourinary Oncology, Dana-Farber Cancer Institute. "With the recent FDA approval of CABOMETYX, patients in need of additional options now have access to a differentiated treatment demonstrated to help them live longer while also delaying the progression of their cancer."

In METEOR, at a median follow-up of nearly 19 months, CABOMETYX demonstrated an increase in median OS of nearly 5 months versus everolimus: 21.4 months versus 16.5 months for everolimus (HR 0.66, 95% CI [0.53-0.83], P=0.0003), corresponding to a 34 percent reduction in the risk of death.

CABOMETYX treatment resulted in consistent benefits in OS and PFS across various pre-specified and post-hoc analysis subgroups. Benefits were independent of Memorial Sloan Kettering Cancer Center risk group (favorable, intermediate, or poor), number and type of prior vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitor (TKI) therapies (one, or more than one), duration of first VEGFR TKI treatment (6 months or less, or more than 6 months), presence of bone and/or visceral metastases, and levels of the MET biomarker in tumors (high, low, or unknown). Additional details on benefits seen in subgroups of patients based on the presence of bone metastases and prior VEGFR TKI therapy will be presented in a poster session at 1 p.m. CDT on June 6.

"We are excited to share the detailed overall survival results from the METEOR trial with the oncology community at this year’s ASCO (Free ASCO Whitepaper) Annual Meeting," said Michael M. Morrissey, Ph.D., president and chief executive officer of Exelixis. "The five-year survival rate for patients diagnosed with advanced kidney cancer is only 12 percent, underscoring the need for new treatment options that help patients live longer while delaying the progression of their disease. Critically, CABOMETYX — the first FDA-approved therapy to demonstrate a benefit in all three key efficacy parameters — now shows consistent survival benefit across all subgroups of patients evaluated in METEOR."

"Recent data from the METEOR trial confirms the benefit in median overall survival of almost 5 months that CABOMETYX can provide to patients with advanced renal cell carcinoma," said Marc de Garidel, Chairman and CEO, Ipsen. "We are dedicated to diligently working with Exelixis and regulatory authorities to bring cabozantinib to patients who seek new therapeutic options with established survival benefits."

At the time of the analysis, the median duration of treatment in the trial was 8.3 months with CABOMETYX versus 4.4 months with everolimus. Dose reductions occurred for 62 percent and 25 percent of patients, respectively. Discontinuation rate due to an adverse event not related to disease progression was 12 percent with CABOMETYX and 11 percent with everolimus.

The most common grade 3 or 4 adverse events were hypertension (15 percent), diarrhea (13 percent) and fatigue (11 percent) in the CABOMETYX arm and anemia (17 percent), fatigue (7 percent) and hyperglycemia (5 percent) in the everolimus arm. Serious adverse events ≥ grade 3 occurred in 130 (39 percent) of cabozantinib-treated patients and in 129 (40 percent) of everolimus-treated patients.

On April 25, 2016 CABOMETYX was approved by the U.S. Food and Drug Administration (FDA) for the treatment of patients with advanced RCC who have received prior anti-angiogenic therapy.

Please see Important Safety Information below and full U.S. prescribing information for CABOMETYX (cabozantinib) tablets at View Source

About the METEOR Phase 3 Pivotal Trial

METEOR was an open-label, event-driven trial of 658 patients with advanced renal cell carcinoma who had failed at least one prior VEGFR TKI therapy. The primary endpoint was PFS in the first 375 patients treated. Secondary endpoints included OS and objective response rate in all enrolled subjects. The trial was conducted at approximately 200 sites in 26 countries, and enrollment was weighted toward Western Europe, North America, and Australia.

Patients were randomized 1:1 to receive 60 mg of CABOMETYX daily or 10 mg of everolimus daily and were stratified based on the number of prior VEGFR TKI therapies received and on MSKCC risk criteria. No cross-over was allowed between the study arms.

METEOR met its primary endpoint of significantly improving PFS. Compared with everolimus, CABOMETYX was associated with a 42 percent reduction in the rate of disease progression or death. Median PFS for CABOMETYX was 7.4 months versus 3.8 months for everolimus (HR=0.58, 95% CI 0.45-0.74, P<0.0001). CABOMETYX also significantly improved the objective response rate compared with everolimus (P<0.0001). These data were presented at the European Cancer Congress in September 2015 and published in The New England Journal of Medicine.2

Exelixis to Host Investor/Analyst Briefing Later Today

Exelixis will host a live investor/analyst briefing today, Sunday, June 5, 2016, from 7:30-9:30 p.m. EDT / 6:30-8:30 p.m. CDT / 4:30-6:30 p.m. PDT. During the briefing, Exelixis management and invited guest speakers will review and provide context for the cabozantinib data presented at the ASCO (Free ASCO Whitepaper) Annual Meeting. The briefing will be webcast live and can be accessed by logging on to www.exelixis.com and proceeding to the Event Calendar page under Investors & Media. Please connect to the company’s website at least 15 minutes prior to the webcast to ensure adequate time for any software download that may be required to listen to the webcast. An archived replay of the webcast will also be available on the Event Calendar page under Investors & Media at www.exelixis.com for one year. A telephone replay of the webcast will be available until 11:59 p.m. EDT on June 7, 2016. Access numbers for the phone replay are: 855-859-2056 (domestic) and 404-537-3406 (international); the passcode is 15007787.

About Advanced Renal Cell Carcinoma

The American Cancer Society’s 2016 statistics cite kidney cancer as among the top ten most commonly diagnosed forms of cancer among both men and women in the U.S.3 Clear cell RCC is the most common type of kidney cancer in adults.4 If detected in its early stages, the five-year survival rate for RCC is high; for patients with advanced or late-stage metastatic RCC, however, the five-year survival rate is only 12 percent, with no identified cure for the disease.3 Approximately 17,000 patients in the U.S. and 37,000 globally require second-line or later treatment.5

The majority of clear cell RCC tumors have lower than normal levels of a protein called von Hippel-Lindau, which leads to higher levels of MET, AXL and VEGF.6,7 These proteins promote tumor angiogenesis (blood vessel growth), growth, invasiveness and metastasis.8-11 MET and AXL may provide escape pathways that drive resistance to VEGFR inhibitors.7,8

About CABOMETYX

CABOMETYX targets include MET, AXL and VEGFR-1, -2 and -3. In preclinical models, cabozantinib has been shown to inhibit the activity of these receptors, which are involved in normal cellular function and pathologic processes such as tumor angiogenesis, invasiveness, metastasis and drug resistance.

CABOMETYX, the tablet formulation of cabozantinib, is available in 20 mg, 40 mg or 60 mg doses. The recommended dose is 60 mg orally, once daily.

On April 25, 2016, the FDA approved CABOMETYX tablets for the treatment of patients with advanced renal cell carcinoma who have received prior anti-angiogenic therapy.

On January 28, 2016, the European Medicines Agency (EMA) validated Exelixis’ Marketing Authorization Application (MAA) for cabozantinib as a treatment for patients with advanced renal cell carcinoma who have received one prior therapy. The MAA has been granted accelerated assessment, making it eligible for a 150-day review, versus the standard 210 days. On February 29, 2016, Exelixis and Ipsen jointly announced an exclusive licensing agreement for the commercialization and further development of cabozantinib indications outside of the United States, Canada and Japan.

Important Safety Information

Hemorrhage: Severe hemorrhage occurred with CABOMETYX. The incidence of Grade ≥3 hemorrhagic events was 2.1% in CABOMETYX-treated patients and 1.6% in everolimus-treated patients. Fatal hemorrhages also occurred in the cabozantinib clinical program. Do not administer CABOMETYX to patients that have or are at risk for severe hemorrhage.

Gastrointestinal (GI) Perforations and Fistulas: Fistulas were reported in 1.2% (including 0.6% anal fistula) of CABOMETYX-treated patients and 0% of everolimus-treated patients. GI perforations were reported in 0.9% of CABOMETYX-treated patients and 0.6% of everolimus-treated patients. Fatal perforations occurred in the cabozantinib clinical program. Monitor patients for symptoms of fistulas and perforations. Discontinue CABOMETYX in patients who experience a fistula that cannot be appropriately managed or a GI perforation.

Thrombotic Events: CABOMETYX treatment results in an increased incidence of thrombotic events. Venous thromboembolism was reported in 7.3% of CABOMETYX-treated patients and 2.5% of everolimus-treated patients. Pulmonary embolism occurred in 3.9% of CABOMETYX-treated patients and 0.3% of everolimus-treated patients. Events of arterial thromboembolism were reported in 0.9% of CABOMETYX-treated patients and 0.3% of everolimus-treated patients. Fatal thrombotic events occurred in the cabozantinib clinical program. Discontinue CABOMETYX in patients who develop an acute myocardial infarction or any other arterial thromboembolic complication.

Hypertension and Hypertensive Crisis: CABOMETYX treatment results in an increased incidence of treatment-emergent hypertension. Hypertension was reported in 37% (15% Grade ≥3) of CABOMETYX-treated patients and 7.1% (3.1% Grade ≥3) of everolimus-treated patients. Monitor blood pressure prior to initiation and regularly during CABOMETYX treatment. Withhold CABOMETYX for hypertension that is not adequately controlled with medical management; when controlled, resume CABOMETYX at a reduced dose. Discontinue CABOMETYX for severe hypertension that cannot be controlled with anti-hypertensive therapy. Discontinue CABOMETYX if there is evidence of hypertensive crisis or severe hypertension despite optimal medical management.

Diarrhea: Diarrhea occurred in 74% of patients treated with CABOMETYX and in 28% of patients treated with everolimus. Grade 3 diarrhea occurred in 11% of CABOMETYX-treated patients and in 2% of everolimus-treated patients. Withhold CABOMETYX in patients who develop intolerable Grade 2 diarrhea or Grade 3-4 diarrhea that cannot be managed with standard antidiarrheal treatments until improvement to Grade 1; resume CABOMETYX at a reduced dose. Dose modification due to diarrhea occurred in 26% of patients.

Palmar-Plantar Erythrodysesthesia Syndrome (PPES): Palmar-plantar erythrodysesthesia syndrome (PPES) occurred in 42% of patients treated with CABOMETYX and in 6% of patients treated with everolimus. Grade 3 PPES occurred in 8.2% of CABOMETYX-treated patients and in <1% of everolimus-treated patients. Withhold CABOMETYX in patients who develop intolerable Grade 2 PPES or Grade 3 PPES until improvement to Grade 1; resume CABOMETYX at a reduced dose. Dose modification due to PPES occurred in 16% of patients.

Reversible Posterior Leukoencephalopathy Syndrome (RPLS): RPLS, a syndrome of subcortical vasogenic edema diagnosed by characteristic finding on MRI, occurred in the cabozantinib clinical program. Perform an evaluation for RPLS in any patient presenting with seizures, headache, visual disturbances, confusion, or altered mental function. Discontinue CABOMETYX in patients who develop RPLS.

Embryo-fetal Toxicity: CABOMETYX can cause fetal harm when administered to a pregnant woman. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with CABOMETYX and for 4 months after the last dose.

Adverse Reactions: The most commonly reported (≥25%) adverse reactions are: diarrhea, fatigue, nausea, decreased appetite, PPES, hypertension, vomiting, weight decreased, and constipation.

Drug Interactions: Strong CYP3A4 inhibitors and inducers: Reduce the dosage of CABOMETYX if concomitant use with strong CYP3A4 inhibitors cannot be avoided. Increase the dosage of CABOMETYX if concomitant use with strong CYP3A4 inducers cannot be avoided.

Lactation: Advise a lactating woman not to breastfeed during treatment with CABOMETYX and for 4 months after the final dose.

Reproductive Potential: Contraception―Advise females of reproductive potential to use effective contraception during treatment with CABOMETYX and for 4 months after the final dose. Infertility ―CABOMETYX may impair fertility in females and males of reproductive potential.

Hepatic Impairment: Reduce the CABOMETYX dose in patients with mild (Child-Pugh score [C-P] A) or moderate (C-P B) hepatic impairment. CABOMETYX is not recommended for use in patients with severe hepatic impairment.

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