KIYATEC Adds Oregon Health & Science University as Study Site for Landmark Clinical Validation Trial of Test to Predict Response to Cancer Therapy Prior to Treatment

On February 6, 2019 KIYATEC, Inc., reported that Oregon Health & Science University (OHSU) Knight Cancer Institute has initiated patient enrollment into KIYATEC’s clinical study, 3D-PREDICT, to validate the company’s test as a patient-specific predictor of response to cancer therapies for solid tumors (Press release, KIYATEC, FEB 6, 2019, View Source [SID1234533099]).

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In this clinical study, the test analyzes a patient’s live cancer cells, grown in KIYATEC’s laboratory within a biologically-relevant 3D microenvironment, to determine whether or not those cells respond to guideline-recommended cancer drugs. Evidence from the company’s earlier pilot study established a correlation between patient-specific predicted tumor response and actual patient clinical response to cancer therapy. The 3D-PREDICT study is a fully prospective, multi-institutional effort to validate the predictive accuracy of the test and correlate response predictions to clinical outcomes among patients with newly diagnosed and relapsed ovarian cancer, glioblastoma and certain rare tumors.

At present, the OHSU Knight Cancer Institute is enrolling newly diagnosed and relapsed ovarian cancer patients into the 3D-PREDICT Study.

"As a pioneer in personalized cancer care, the OHSU Knight Cancer Institute is deeply committed to optimizing appropriate therapy for our patients as early as possible following diagnosis, when the disease is most treatable," said Dr. Koen De Geest, lead investigator of the clinical trial at OHSU. "Five-year survival among high-grade ovarian cancer patients is 30%, and we believe this test has the potential to help improve outcomes in the clinic."

"With cancer treatment, and especially ovarian cancer, time is of the essence and being able to measure patient-specific evidence of response and non-response before treatment begins can truly change the future of cancer care," said Matthew Gevaert, CEO of KIYATEC. "We welcome OHSU to our clinical study and their participation will be integral as we work to deliver accurate predictions of patient response to cancer therapies, reducing the need for patients to undergo treatments that may not work."

The 3D-PREDICT study is anticipated to continue through 2022. Details on the trial can be found on View Source

Pathios Therapeutics and Sygnature Discovery sign a strategic and innovative partnership to develop first-in-class therapies.

On February 6, 2019 Pathios Therapeutics ("Pathios"), an innovative biotech company focused on the development of first in class therapies for autoimmune diseases and immuno-oncology and Sygnature Discovery ("Sygnature"), reported a strategic partnership to accelerate Pathios’ drug discovery and development programmes (Press release, Pathios Therapeutics, FEB 6, 2019, View Source [SID1234650160]).

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As part of the agreement, Pathios and Sygnature will collaborate on an integrated drug discovery programme against a novel G Protein-Coupled Receptor (GPCR) target. Specifically, Sygnature are providing their industry leading expertise in GPCR bioscience and medicinal chemistry to expand Pathios’ current hit-to-lead programme. Sygnature are also deploying their computational chemistry, library design and synthesis and medium throughput screening capability to broaden Pathios’ hit finding. As part of this agreement, Sygnature will receive equity in addition to fees.

Pathios Therapeutics brings together cutting-edge European science and a leading drug discovery and development team to modulate the activity of GPR65, a pH sensing GPCR. This drug target is characteristic of certain T helper 17 (Th17) cell populations which have been shown to contribute significantly to the pathology of autoimmune conditions, such as ankylosing spondylitis and psoriatic arthritis. In addition, recently published studies have demonstrated GPR65 drives tumour associated macrophages (TAM) to adopt a phenotype that supports cancer immune evasion.

Tom McCarthy, Executive Chairman and Co-founder of Pathios Therapeutics Limited, commented: "We founded Pathios to build on emerging science that demonstrated GPR65 sits at the nexus of autoimmune disease and immuno-oncology as this receptor links pathology caused by a low pH environment. The ultimate aim is to block the pathological process that GPR65 initiates without interfering with the physiological role of this receptor. In addition to developing potent and selective drugs to modulate GPR65, we are continuing to broaden the understanding of the fundamental biological processes that link to GPR65’s effects in Th17 cells, TAMs and other cell types. Our team has worked closely with Sygnature in the past and know they have the deep experience, expertise and state-of-the-art drug discovery and development infrastructure to drive our programme forward. I’m delighted on this rare occasion Sygnature also chose to invest in Pathios and expand our GPR65 drug discovery efforts while we explore Series A funding opportunities".

Simon Hirst, CEO of Sygnature, added: "We are extremely pleased to take this exceptional opportunity to partner with, and invest in Pathios on their drug discovery projects. Based on our diligence activities, we are excited about the potential for GPR65 modulation to be central to new treatments for autoimmune disease and a critical mechanism of action in next generation immunooncology drugs targeting the tumour micro-environment. We are excited to have the opportunity to work with Tom and the rest of Pathios’ tremendously talented team again and contribute to the potential positive impact their therapeutics will have on patients’ lives".

Arch Oncology Announces First Patient Dosed in Phase 1 Clinical Trial of AO-176, an Anti-CD47 Antibody with a Best-in-Class Profile

On February 6, 2019 Arch Oncology, Inc., a clinical-stage immuno-oncology company focused on the discovery and development of next-generation anti-CD47 antibody therapies for cancer, reported the initiation of a new Phase 1 clinical trial of AO-176 in select solid tumors with the first patient dosed (Press release, Arch Oncology, FEB 6, 2019, View Source [SID1234533100]). AO-176 is an anti-CD47 antibody with a best-in-class profile that works by blocking the "don’t eat me" signal and also by directly killing tumor cells, with preferential binding to tumor versus normal cells.

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"Dosing the first patient in this new trial is a significant milestone for our Company," said Julie M. Cherrington, Ph.D., President and Chief Executive Officer of Arch Oncology. "AO-176 is an anti-CD47 antibody with a best-in-class profile and we are excited to be part of the effort to advance this new class of therapeutics. Our team has worked diligently to bring AO-176 into the clinic, and our aim is to develop this antibody as a new treatment approach for patients with cancer."

Howard A. "Skip" Burris, III, M.D., President, Clinical Operations, Chief Medical Officer, and Principal Investigator, Sarah Cannon Research Institute, commented, "There is a growing body of research on AO-176, which has demonstrated in preclinical studies a highly differentiated mechanism among the anti-CD47 agents. With greater insights into the number of tumors that overexpress CD47, we are excited to participate in this study to assess this next-generation anti-CD47 antibody’s safety and preliminary efficacy profile."

Sarah Cannon Research Institute dosed the first patient in the Phase 1 clinical trial of AO-176. The multicenter, open-label, dose-escalation and dose-expansion study is evaluating the safety, pharmacokinetics, pharmacodynamics, and preliminary anti-tumor activity of AO-176 in patients with select solid tumors.

About AO-176

AO-176 is a humanized anti-CD47 IgG2 antibody with a best-in-class profile. Arch Oncology’s next-generation anti-CD47 antibody AO-176 is highly differentiated, with the potential to improve upon the safety and efficacy profile relative to other agents in this class of checkpoint inhibitors. AO-176 works by blocking the "don’t eat me" signal, the standard mechanism of anti-CD47 antibodies. Beyond blocking this signal, AO-176 also works by directly killing tumor cells. Importantly, AO-176 binds preferentially to tumor cells, instead of to normal cells, and binds even more potently to tumors in their acidic microenvironment (low pH). AO-176 is in a Phase 1 clinical trial for the treatment of patients with select solid tumors.

Data presented on AO-176 at recent medical and scientific meetings can be found at View Source

Vaxart Announces Fourth Quarter and Year-End 2018 Financial Results and Provides Corporate Update

On February 6, 2019 Vaxart, Inc., a clinical-stage biotechnology company developing oral recombinant vaccines that are administered by tablet rather than by injection, reported financial results for the fourth quarter and full year ended December 31, 2018 (Press release, Vaxart, FEB 6, 2019, View Source [SID1234533101]).

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"As we execute on our objective of building a leading oral vaccine company, we continue to expand our understanding of the unique properties of our oral vaccine platform and the important advantages we believe it can offer over conventional injectable vaccines, particularly for mucosal pathogens such as norovirus, flu and RSV," said Wouter Latour, M.D., chief executive officer of Vaxart. "We are focused on our lead product candidate, the first oral vaccine against norovirus, a disease with a $34 billion economic impact in high income countries including the United States, Europe and Japan. After laying the groundwork in 2018, we expect to initiate our norovirus Phase 1 bivalent study and Phase 2 monovalent challenge study during the first half of 2019. In parallel, we are advancing our first therapeutic vaccine targeting HPV-associated dysplasia and cancer toward the clinic."

2018 Highlights:

Corporate:

In February, Vaxart commenced trading on the Nasdaq Capital Market under the symbol "VXRT" following the closing of its merger with Aviragen Therapeutics.
In October, at ID Week in San Francisco, the Company presented data from its H1 influenza Phase 2 challenge study demonstrating that its oral H1 flu vaccine, while providing 39% reduction in flu illness compared to 27% for Fluzone, protected primarily through mucosal immunity, in contrast to Fluzone which primarily protected through serum antibodies. This finding provides evidence that Vaxart’s oral vaccines may deliver better protection against mucosal pathogens than injectable vaccines.
In July, Vaxart announced the publication of the comprehensive results of the previously disclosed Phase 1 clinical trial with its norovirus oral tablet vaccine in the Journal of Clinical Investigation Insight. As reported in the article, the vaccine generated robust systemic and mucosal immune responses, including mucosal IgA, memory B cells, and serum blocking antibody titers (BT50), all potential correlates of protection.
In October at the 32nd International Papillomavirus Conference, the Company presented preclinical data on its human papillomavirus (HPV) vaccine trial. The Vaxart HPV vaccine created CD8 tumor-infiltrating T cells and eliminated or significantly reduced the majority of tumors with or without a checkpoint inhibitor.
In June, the Company announced the publication of preclinical results from its oral F-protein based Respiratory Syncytial Virus (RSV-F) vaccine in Vaccine. As described in the article, the oral RSV-F vaccine candidate provided complete sterilizing protection against RSV infection in the cotton rat challenge model at the target dose.
Financial Results for the Three Months and Year Ended December 31, 2018

Vaxart reported a net loss of $4.9 million for the fourth quarter of 2018 compared to a net loss of $1.1 million for the fourth quarter of 2017. For the year ended December 31, 2018, the net loss was $18.0 million compared to a net loss of $9.6 million for 2017.
Vaxart ended the year with cash and cash equivalents of $11.5 million compared to $17.9 million at September 30, 2018. The decrease was primarily due to cash used in operations.
Revenue for the quarter was $1.8 million compared to $0.8 million in the fourth quarter of 2017. The increase was due to royalty revenue resulting from our merger with Aviragen, offset by lower revenues from the contract with BARDA, which ended on September 30, 2018.
Research and development expenses were $4.5 million for the quarter compared to $1.9 million for the fourth quarter of 2017. The increase was mainly due to higher clinical and manufacturing costs incurred in the Company’s norovirus program and amortization of intangible assets acquired in the merger with Aviragen, offset by lower expenditures incurred under the BARDA contract.
General and administrative expenses were $1.2 million for the quarter compared to $1.5 million for the fourth quarter of 2017. The decrease was a result of significant one-off costs incurred in the 2017 period in connection with the merger with Aviragen

ARRAY BIOPHARMA REPORTS FINANCIAL RESULTS FOR THE SECOND QUARTER OF FISCAL 2019

On February 5, 2019 Array BioPharma Inc. (Nasdaq: ARRY) reported results for its second quarter of fiscal 2019 and provided an update on the progress of its key commercial products and clinical development programs (Press release, Array BioPharma, FEB 5, 2019, View Source [SID1234533068]).

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"We continue to be pleased with demand following the U.S. launch of BRAFTOVI + MEKTOVI for patients with BRAF-mutant metastatic melanoma, which delivered $22.7 million in net product sales during the second commercial quarter," said Ron Squarer, Chief Executive Officer. "Separately, we were excited to report an unprecedented 15.3 months mature median overall survival from the safety lead-in of the Phase 3 BEACON CRC trial and we recently completed enrollment of the randomized portion of the trial. We look forward to the interim analysis in the first half of 2019."

MELANOMA
COMMERCIAL
U.S. Sales
BRAFTOVI + MEKTOVI net product sales for the second quarter was $22.7 million, which represents quarter over quarter growth of 62%. Feedback from prescribers continues to be positive.

European Launch
BRAFTOVI + MEKTOVI has launched in Germany, Austria, the Netherlands and the United Kingdom. Preparations for launch in other countries are under way.

Japanese Approval
On January 8, 2019, BRAFTOVI + MEKTOVI received manufacturing and marketing approval in Japan for the indication of unresectable melanoma with a BRAF mutation.

COLORECTAL CANCER (CRC)
BEACON CRC PHASE 3 TRIAL
Safety Lead-in Median Overall Survival (OS) Data Presented at ASCO (Free ASCO Whitepaper) 2019 Gastrointestinal Cancers Symposium
Array announced updated safety and efficacy results from the safety lead-in of the Phase 3 BEACON CRC trial evaluating the triplet combination of BRAFTOVI, MEKTOVI, and ERBITUX in patients with BRAFV600E-mutant metastatic colorectal cancer (mCRC).

Mature median OS was 15.3 months (95% CI, 9.6–not reached) for patients treated with the triplet.
Updated median progression-fee survival (mPFS) and updated confirmed overall response rate (ORR) results for patients treated with the triplet in the safety lead-in remain the same, as previously reported, with 8 months mPFS (95% CI, 5.6-9.3) and a 48% ORR (95% CI, 29.4–67.5). Overall response rate by central assessment, 41% (95% CI 24%–61%), was consistent with local assessment.
The triplet combination was generally well-tolerated with no unexpected toxicities. The most common grade 3 or 4 adverse events seen in at least 10% of patients were fatigue (13%), anemia (10%), increased creatine phosphokinase (10%), increased aspartate aminotransferase (10%) and urinary tract infections (10%). The rate of grade 3 or 4 skin toxicities continued to be lower than generally observed with ERBITUX in mCRC.
Breakthrough Therapy Designation
On August 7, 2018, Array announced that the FDA granted Breakthrough Therapy Designation to BRAFTOVI, in combination with MEKTOVI and ERBITUX for the treatment of patients with BRAFV600E-mutant mCRC as detected by an FDA-approved test, after failure of one to two prior lines of therapy for metastatic disease. BRAFV600E-mutant mCRC patients have a mortality risk more than double that of mCRC patients without the mutation, and currently there are no therapies specifically approved for this high unmet need population. [1-8]

Regulatory Update
Following consultation with the FDA and European Medicines Agency, Array has initiated an amendment to the BEACON CRC protocol to allow for an interim analysis of trial endpoints. Should a planned analysis based primarily on confirmed ORR and durability of response be supportive, the Company plans to use it to seek accelerated approval in the U.S. The interim analysis may also support regulatory submissions in other regions. The Company anticipates topline results from this analysis in the first half of 2019. This timing allows for the subset of patients required for the interim analysis of ORR to achieve a response and for the durability of responses to be appropriately evaluated. The BEACON CRC trial has completed enrollment.

ANCHOR CRC TRIAL
ANCHOR CRC, an international trial designed to assess the efficacy and safety of the combination of BRAFTOVI, MEKTOVI, and ERBITUX in patients with BRAFV600E-mutant mCRC in the first-line setting, is advancing. This trial was designed in partnership with top global key opinion leaders and Array is excited by the potential of this combination therapy to benefit patients in the first-line setting. The ANCHOR CRC trial is being conducted in collaboration with Pierre Fabre and Ono Pharmaceutical Co., Ltd., and with support from Merck KGaA, Darmstadt, Germany (support is for sites outside of North America).

IMMUNO-ONCOLOGY COLLABORATIONS
TRIALS ADVANCING WITH BRISTOL-MYERS SQUIBB, MERCK AND PFIZER
Array is developing MEKTOVI in combination with PD-1/PD-L1 checkpoint inhibitors and previously announced separate, strategic collaborations with Bristol-Myers Squibb, Merck and Pfizer. Each collaboration is pursuing a different rationally designed clinical approach in several solid tumor populations including mCRC patients with microsatellite stable tumors (BMS and Merck), and patients with non-small cell lung and pancreatic cancer (Pfizer). These approaches are characterized by their focus on earlier lines of therapy and the addition of a third regimen.

FINANCIAL HIGHLIGHTS

Second Quarter of Fiscal 2019 Compared to First Quarter of Fiscal 2019

Net Product Sales for BRAFTOVI + MEKTOVI for the second quarter of fiscal 2019 was $22.7 million, compared to $14.0 million for the first quarter of fiscal 2019.
Total Revenue for the second quarter of fiscal 2019 was $82.5 million, compared to $56.9 million for the prior quarter. The increase was primarily due to higher product sales and recognition of $40 million of milestone revenue from Loxo Oncology, which was partially offset by reduced reimbursement revenue from Novartis and milestones earned in the previous quarter.
Cost of Goods Sold related to our product revenues for the second quarter of fiscal 2019 was $0.8 million which represents 3.5% of net sales, compared to $0.2 million for the prior quarter.
Research and development expense for proprietary programs for the second quarter of fiscal 2019 was $62.1 million, compared to $55.6 million for the prior quarter. The increase was primarily driven by proprietary trial activities including the BEACON CRC trial, which was partially offset by lower activity on the Novartis transitioned studies.
Selling, General and Administrative for the second quarter of fiscal 2019 was $30.5 million, compared to $24.9 million for the prior quarter. The increase was mostly driven by costs associated with BRAFTOVI + MEKTOVI commercial and sales activities.
Net loss for the second quarter of fiscal 2019 was $11.4 million, or ($0.05) per share, compared to $24.8 million, or ($0.12) per share, for the prior quarter. The decrease in net loss was primarily due to increased product sales and increased milestone revenue from Loxo Oncology, which was partially offset by increased operating expenses and reduced reimbursement revenue from Novartis.
Cash, cash equivalents and marketable securities as of December 31, 2018 were $478 million.
CONFERENCE CALL INFORMATION
Array will hold a conference call on Tuesday, February 5, 2019, at 9:00 a.m. Eastern Time to discuss these results and provide an update on the progress of its key commercial products and clinical development programs. Ron Squarer, Chief Executive Officer, will lead the call.

Date:

Tuesday, February 5, 2019

Time:

9:00 a.m. Eastern Time

Toll-Free:

(844) 464-3927

Toll:

(765) 507-2598

Pass Code:

9778144

Webcast, including Replay and Conference Call Slides:
View Source

About BRAF-mutant Metastatic Melanoma
Melanoma develops when unrepaired DNA damage to skin cells triggers mutations that may lead them to multiply and form malignant tumors. Metastatic melanoma is the most serious and life-threatening type of skin cancer and is associated with low survival rates. [9,10] There are a variety of gene mutations that can lead to metastatic melanoma. The most common genetic mutation in metastatic melanoma is BRAF. There are about 200,000 new cases of melanoma diagnosed worldwide each year, approximately half of which have BRAF mutations, a key target in the treatment of metastatic melanoma. [9-13]

About BRAFTOVI + MEKTOVI
BRAFTOVI is an oral small molecule BRAF kinase inhibitor and MEKTOVI is an oral small molecule MEK inhibitor which target key enzymes in the MAPK signaling pathway (RAS-RAF-MEK-ERK). Inappropriate activation of proteins in this pathway has been shown to occur in many cancers including melanoma, colorectal cancer, non-small cell lung cancer and others. In the U.S., BRAFTOVI + MEKTOVI are approved for the treatment of unresectable or metastatic melanoma with a BRAFV600E or BRAFV600K mutation, as detected by an FDA-approved test. BRAFTOVI is not indicated for treatment of patients with wild-type BRAF melanoma. In Europe, the combination is approved for adult patients with unresectable or metastatic melanoma with a BRAFV600mutation, as detected by a validated test.

Array has exclusive rights to BRAFTOVI and MEKTOVI in the U.S. and Canada. Array has granted Ono Pharmaceutical Co., Ltd., exclusive rights to commercialize both products in Japan and South Korea, Medison exclusive rights to commercialize both products in Israel and Pierre Fabre exclusive rights to commercialize both products in all other countries, including Europe, Latin American and Asia (excluding Japan and South Korea).

BRAFTOVI + MEKTOVI have received regulatory approval in the U.S., European Union, Australia and Japan. The Swiss Medicines Agency (Swissmedic) is currently reviewing the Marketing Authorization Applications for BRAFTOVI and MEKTOVI submitted by Pierre Fabre.

Indications and Usage
BRAFTOVI (encorafenib) and MEKTOVI (binimetinib) are kinase inhibitors indicated for use in combination for the treatment of patients with unresectable or metastatic melanoma with a BRAFV600E or BRAFV600K mutation, as detected by an FDA-approved test.

Limitations of Use: BRAFTOVI is not indicated for the treatment of patients with wild-type BRAF melanoma.

BRAFTOVI + MEKTOVI Important Safety Information
The information below applies to the safety of the combination of BRAFTOVI and MEKTOVI unless otherwise noted. See full Prescribing Information for BRAFTOVI and for MEKTOVI for dose modifications for adverse reactions.

Warnings and Precautions
New Primary Malignancies: Cutaneous and non-cutaneous malignancies can occur. In the COLUMBUS trial, cutaneous squamous cell carcinoma, including keratoacanthoma, occurred in 2.6% and basal cell carcinoma occurred in 1.6% of patients. Perform dermatologic evaluations prior to initiating treatment, every 2 months during treatment, and for up to 6 months following discontinuation of treatment. Manage suspicious skin lesions with excision and dermatopathologic evaluation. Dose modification is not recommended for new primary cutaneous malignancies. Based on its mechanism of action, BRAFTOVI may promote malignancies associated with activation of RAS through mutation or other mechanisms. Monitor patients receiving BRAFTOVI for signs and symptoms of non-cutaneous malignancies. Discontinue BRAFTOVI for RAS mutation-positive non-cutaneous malignancies.

Tumor Promotion in BRAF Wild-Type Tumors: Confirm evidence of BRAFV600E or V600K mutation prior to initiating BRAFTOVI.

Cardiomyopathy, manifesting as left ventricular dysfunction associated with symptomatic or asymptomatic decreases in ejection fraction, has been reported in patients. In the COLUMBUS trial, cardiomyopathy occurred in 7% and Grade 3 left ventricular dysfunction occurred in 1.6% of patients. Cardiomyopathy resolved in 87% of patients. Assess left ventricular ejection fraction by echocardiogram or MUGA scan prior to initiating treatment, 1 month after initiating treatment, and then every 2 to 3 months during treatment. Safety has not been established in patients with a baseline ejection fraction that is either below 50% or below the institutional lower limit of normal. Patients with cardiovascular risk factors should be monitored closely.

Venous Thromboembolism (VTE): In the COLUMBUS trial, VTE occurred in 6% of patients, including 3.1% of patients who developed pulmonary embolism.

Hemorrhage: In the COLUMBUS trial, hemorrhage occurred in 19% of patients and ≥ Grade 3 hemorrhage occurred in 3.2% of patients. Fatal intracranial hemorrhage in the setting of new or progressive brain metastases occurred in 1.6% of patients. The most frequent hemorrhagic events were gastrointestinal, including rectal hemorrhage (4.2%), hematochezia (3.1%), and hemorrhoidal hemorrhage (1%).

Ocular Toxicities: In the COLUMBUS trial, serous retinopathy occurred in 20% of patients; 8% were retinal detachment and 6% were macular edema. Symptomatic serous retinopathy occurred in 8% of patients with no cases of blindness. RVO is a known class-related adverse reaction of MEK inhibitors and may occur in patients treated with MEKTOVI in combination with encorafenib. In patients with BRAF mutation-positive melanoma across multiple clinical trials, 0.1% of patients experienced retinal vein occlusion (RVO). The safety of MEKTOVI has not been established in patients with a history of RVO or current risk factors for RVO including uncontrolled glaucoma or a history of hyperviscosity or hypercoagulability syndromes. Perform ophthalmological evaluation for patient-reported acute vision loss or other visual disturbance within 24 hours. Permanently discontinue MEKTOVI in patients with documented RVO. In COLUMBUS, uveitis, including iritis and iridocyclitis was reported in 4% of patients. Assess for visual symptoms at each visit. Perform ophthalmological evaluation at regular intervals and for any visual disturbances, and to follow new or persistent ophthalmologic findings.

Interstitial Lung Disease (ILD): ILD, including pneumonitis occurred in 0.3% of patients with BRAF mutation-positive melanoma across multiple clinical trials. Assess new or progressive unexplained pulmonary symptoms or findings for possible ILD.

Hepatotoxicity: In the COLUMBUS trial, the incidence of Grade 3 or 4 increases in liver function laboratory tests was 6% for alanine aminotransferase (ALT) and 2.6% for aspartate aminotransferase (AST), and 0.5% for alkaline phosphatase. Monitor liver laboratory tests before and during treatment and as clinically indicated.

Rhabdomyolysis: In the COLUMBUS trial, elevation of laboratory values of serum creatine phosphokinase (CPK) occurred in 58% of patients. Rhabdomyolysis was reported in 0.1% of patients with BRAF mutation-positive melanoma across multiple clinical trials. Monitor CPK and creatinine levels prior to initiating MEKTOVI, periodically during treatment, and as clinically indicated.

QTc Prolongation: BRAFTOVI is associated with dose-dependent QTc interval prolongation in some patients. In the COLUMBUS trial, an increase in QTcF to > 500 ms was measured in 0.5% (1/192) of patients. Monitor patients who already have or who are at significant risk of developing QTc prolongation. Correct hypokalemia and hypomagnesemia prior to and during BRAFTOVI administration. Withhold, reduce dose, or permanently discontinue for QTc > 500 ms.

Embryo-Fetal Toxicity: BRAFTOVI or MEKTOVI can cause fetal harm when administered to pregnant women. BRAFTOVI can render hormonal contraceptives ineffective. Non-hormonal contraceptives should be used during treatment and for at least 30 days after the final dose for patients taking BRAFTOVI + MEKTOVI.

Adverse Reactions
The most common adverse reactions (≥20%, all Grades, in the COLUMBUS trial): were fatigue, nausea, diarrhea, vomiting, abdominal pain, arthralgia, myopathy, hyperkeratosis, rash, headache, constipation, visual impairment, serous retinopathy.

In the COLUMBUS trial, the most common laboratory abnormalities (≥20%, all Grades): included increased creatinine, increased CPK, increased gamma glutamyl transferase, anemia, increased ALT, hyperglycemia, increased AST, and increased alkaline phosphatase.

Drug Interactions
Avoid concomitant use of strong or moderate CYP3A4 inhibitors or inducers and sensitive CYP3A4 substrates with BRAFTOVI. Modify BRAFTOVI dose if concomitant use of strong or moderate CYP3A4 inhibitors cannot be avoided. Avoid co-administration of BRAFTOVI with medicinal products with a known potential to prolong QT/QTc interval.

Please see full Prescribing Information for BRAFTOVI and full Prescribing Information for MEKTOVI for additional information. [14,15] You may report side effects to the FDA at (800) FDA-1088 or www.fda.gov/medwatch. You may also report side effects to Array at 1-844-Rx-Array (1-844-792-7729).

About Colorectal Cancer
Worldwide, colorectal cancer is the third most common type of cancer in men and the second most common in women, with approximately 1.4 million new diagnoses in 2012. Globally in 2012, approximately 694,000 deaths were attributed to colorectal cancer. [16] In the U.S. alone, an estimated 140,250 patients will be diagnosed with cancer of the colon or rectum in 2018, and approximately 50,000 are estimated to die of their disease. [17] BRAF mutations are estimated to occur in up to 15% of patients with mCRC and represent a poor prognosis for these patients. [1-3, 18-19] The V600 mutation is the most common BRAF mutation and the risk of mortality in CRC patients with the BRAFV600E mutation is more than two times higher than for those with wild-type BRAF. [8,18] Several irinotecan and cetuximab-containing regimens, similar to the BEACON CRC control arm, have established observed historical published benchmarks in BRAFV600E-mutant mCRC patients, whose disease has progressed after one or two prior lines of therapy. These benchmarks include ORR of 4% to 8%, mPFS of 2 to 3 months and median OS of 4 to 6 months. [1-7,20] BRAF V600E-mutant mCRC is an area of high unmet need as there are currently no FDA-approved therapies specifically indicated for patients with BRAF-mutant mCRC, and these patients derive limited benefit from available chemotherapy regimens. [21-23] For more information about BRAFV600E-mutant mCRC visit www.brafmcrc.com.

About BEACON CRC
BEACON CRC is a randomized, open-label, global trial evaluating the efficacy and safety of BRAFTOVI, MEKTOVI and ERBITUX in patients with BRAFV600E-mutant mCRC whose disease has progressed after one or two prior regimens. BEACON CRC is the first and only Phase 3 trial designed to test a BRAF/MEK combo targeted therapy in BRAFV600E-mutant mCRC. Thirty patients were treated in the safety lead-in and received the triplet combination (BRAFTOVI 300 mg daily, MEKTOVI 45 mg twice daily and ERBITUX per label). Of the 30 patients, 29 had a BRAFV600 mutation. MSI-H, resulting from defective DNA mismatch repair, was detected in only 1 patient. As previously announced, the triplet combination demonstrated good tolerability, supporting initiation of the randomized portion of the trial. The randomized portion of the BEACON CRC trial is designed to assess the efficacy of BRAFTOVI in combination with ERBITUX with or without MEKTOVI compared to ERBITUX and irinotecan-based therapy. Approximately 615 patients are expected to be randomized 1:1:1 to receive triplet combination, doublet combination (BRAFTOVI and ERBITUX) or the control arm (irinotecan-based therapy and ERBITUX). The study has been amended to include an interim analysis of endpoints including ORR. The primary overall survival endpoint is a comparison of the triplet combination to the control arm. Secondary endpoints address efficacy of the doublet combination compared to the control arm, and the triplet combination compared to the doublet therapy. Other secondary endpoints include PFS, duration of response, safety and tolerability. Health related quality of life data will also be assessed. The trial is being conducted at over 200 investigational sites in North America, South America, Europe and the Asia Pacific region. The BEACON CRC trial is being conducted with support from Ono Pharmaceutical Co. Ltd., Pierre Fabre and Merck KGaA, Darmstadt, Germany (support is for sites outside of North America).

The triplet combination of BRAFTOVI, MEKTOVI and ERBITUX for the treatment of patients with BRAFV600E-mutant mCRC is investigational and not approved by the FDA.