Targeting BTK with Ibrutinib in Relapsed or Refractory Mantle-Cell Lymphoma

SUMMARY:The FDA granted accelerated approval to Ibrutinib (IMBRUVICA®), for the treatment of patients with Mantle Cell Lymphoma (MCL), who had received at least one prior therapy. Bruton's Tyrosine Kinase (BTK) is a cytoplasmic protein predominantly expressed in B-cells and is a mediator of B-cell receptor signaling in normal and transformed B-cells. BTK is necessary for the proliferation and survival of B-cell tumors. IMBRUVICA® is an oral, irreversible inhibitor of BTK and thereby inhibits cell proliferation and promotes programmed cell death (Apoptosis). The efficacy of IMBRUVICA® was evaluated in a multi-center, international, single-arm Phase II trial in which 111 patients with previously treated MCL, received IMBRUVICA®, at a daily oral dose of 560 mg. The median age was 68 years and patients had received a median of three prior therapies. Patients were stratified into those who had previously received at least 2 cycles of VELCADE® (Bortezomib) therapy and those who had received less than 2 cycles or had no prior therapy with VELCADE®. More than 80% of patients had intermediate-risk or high-risk disease. Treatment was given until disease progression or until unacceptable toxicities were noted. The primary end point was Overall Response Rate (ORR). Secondary end points included duration of response, Progression Free Survival (PFS), Overall Survival (OS), and safety. With a median follow-up of 15.3 months, the ORR was 68%, with a 21% Complete Response and 47% Partial Response rate. The estimated median duration of response was 17.5 months. Prior treatment with VELCADE® had no influence on the Response Rate (RR). The median PFS was 13.9 months and estimated OS was 58% at 18 months. Treatment related toxicities were mild to moderate nausea, diarrhea, fatigue, and cytopenias. Grade 3 bleeding was noted in 5% of the patients, but these patients had a history of falls and were receiving either Aspirin or Warfarin. The authors concluded that IMBRUVICA® given as a single agent has durable efficacy in relapsed or refractory MCL. Studies are underway, combining IMBRUVICA® with TREANDA® (Bendamustine) and RITUXAN® (Rituximab), as front line therapy for patients with MCL. The list of agents for the treatment of relapsed or refractory MCL now include VELCADE®, REVLIMID® and IMBRUVICA®. Wang ML, Rule S, Martin P, et al. N Engl J Med 2013; 369:507-516

Results of Initial Low-Dose Computed Tomographic Screening for Lung Cancer

SUMMARY: The National Lung Screening Trial (NLST), a federally funded U.S. study, enrolled 53,439 asymptomatic participants, 55 to 74 years of age, with at least 30 pack-year smoking history, and were randomized to undergo annual screening with either low dose CT scan (n=26,715) or a chest X-Ray (n=26,724), for three years. The use of low dose CT scans for 3 years in this high risk, healthy patients, resulted in a 20% reduction in Lung Cancer mortality, compared to screening with a chest X-Ray. Based on these findings, Lung Cancer Screening is recommended for the following groups

1) People 55-74 years of age with no signs or symptoms of Lung Cancer

2) Current or former smoker with a 30 pack year smoking history (Number of years smoked multiplied by the number of packs of cigarettes per day)

3) Current smokers are strongly urged to enter a smoking cessation program

4) Former smokers must have quit smoking within the past 15 years

Lung Cancer screening is performed using a non-contrast, low dose CT scan. People with serious co-morbid conditions, those on home oxygen and individuals with metallic devices or implants in the chest or back (which can interfere with the scan) should be excluded from Lung Cancer screening. It should be noted that Lung cancer screening with low dose CT scan is presently not covered by most insurance plans. The National Lung Screening Trial Research Team. N Engl J Med 2013;368:1980-1991

Pomalidomide plus low-dose dexamethasone versus high-dose dexamethasone alone for patients with relapsed and refractory multiple myeloma (MM-003) a randomised, open-label, phase 3 trial

SUMMARY: Pomalidomide (POMALYST®) is a novel, oral, immunomodulatory agent which is far more potent than Thalidomide (THALOMID®) and Lenalidomide (REVLIMID®). Only 2% of POMALYST® is excreted unchanged through the kidney whereas 80% of REVLIMID® is excreted unchanged via the kidneys. Therefore, POMALYST® may be a consideration for patients with renal insufficiency. Previously conducted phase II trials have shown POMALYST® to be active in Myeloma patients, refractory to REVLIMID® and Bortezomib (VELCADE®). In a multicenter, randomized, phase III trial, the efficacy and safety of POMALYST® given along with low-dose Dexamethasone (LoDEX) (n=302) was compared with high-dose Dexamethasone (HiDEX) (n=153) in Myeloma patients, who were refractory to both REVLIMID® and VELCADE®. The primary endpoint was Progression Free Survival (PFS). The Overall Survival (OS) was only evaluated if PFS was statistically significant. With a median follow up of 10 months, the PFS was significantly longer in the POMALYST® + LoDEX group compared to the HiDEX group (4 month vs 1.9 months; hazard ratio [HR]= 0.48; P <0 .0001). The median OS was significantly longer in the POMALYST® + LoDEX group compared to HiDEX group (12.7 months vs 8.1 months; HR=0.74; P=0.028). The authors concluded that POMALYST® along with low- dose Dexamethasone should be the new standard of care for patients who have Multiple Myeloma refractory to REVLIMID® and VELCADE®. Carfilzomib (KYPROLIS®), a new parenteral proteasome inhibitor is another option for patients with resistant and refractory Multiple Myeloma. San Miguel J, Weisel K, Moreau P, et al. Lancet Oncol 2013;14:1055-1066

Adjuvant Chemotherapy With Gemcitabine and Long-term Outcomes Among Patients With Resected Pancreatic Cancer

SUMMARY: Curative surgical resection has been shown to significantly improve Overall Survival (OS) when compared to Chemoradiation, for resectable Pancreatic Cancer. The standard surgical procedure for tumors of the Pancreatic head is the Pancreaticoduodenectomy (Whipple procedure), whereas distal Pancreatectomy is performed for tumors of the body or tail of the Pancreas. The role of adjuvant chemotherapy following surgery has however remained unclear. In this community based, phase III trial, 368 patients were randomly assigned to receive either adjuvant chemotherapy with GEMZAR® (Gemcitabine) (N=186) or Observation (N=182), following curative resection of the pancreas (Macroscopic complete removal of Pancreatic cancer). Chemotherapy consisted of 6 cycles of GEMZAR® with each cycle consisting of GEMZAR® 1000mg/m2, given weekly, 3 out of 4 weeks. Patients were stratified based on tumor stage (T), nodal status (N) and resection (R) status. The primary endpoint was Disease Free Survival (DFS). Secondary endpoints included OS and safety. With a median follow up of 136 months, the median DFS was 13.4 months in the treatment group vs 6.7 months in the observation group (HR=0.55; P<0.001). The OS in the treatment group was significantly prolonged (HR=0.76; P=0.01), with a 5 year survival of 21% and 10 year survival of 12% compared to 10% and 8% respectively, in the Observation group. The authors concluded that 6 months of GEMZAR® based adjuvant therapy improves Overall Survival for patients with resectable Pancreatic Cancer. There may be added benefit with regimens associated with higher remission rates such as FOLFIRINOX or weekly ABRAXANE® (Paclitaxel albumin-bound particles) and GEMZAR®. Oettle H, Neuhaus P, Hochhaus A, et al. JAMA. 2013;310:1473-1481.

Subcutaneous Omacetaxine Mepesuccinate in Patients With Chronic-Phase Chronic Myeloid Leukemia Previously Treated With 2 or More Tyrosine Kinase Inhibitors Including Imatinib

SUMMARY: Omacetaxine Mepesuccinate (SYNRIBO®) is a first-in-class cephalotaxine and is a semi synthetic purified Homoharringtonine (HHT) compound. HHT is a plant alkaloid derived from Cephalotaxus fortunei, a coniferous bush, also called Japanese Plum Yew. With over 40 years of drug development history since its discovery, SYNRIBO®, unlike Tyrosine Kinase Inhibitors (TKI), is a protein synthesis inhibitor and reduces the levels of multiple Oncoproteins including BCR-ABL, BCL-2, MCL-1 and promotes apoptosis of leukemic stem cells. The following is the pooled data from 2 phase II trials. Treatment population included patients with Chronic Myeloid Leukemia – Chronic Phase (CML-CP), resistant or intolerant to GLEEVEC® (Imatinib) and at least one other TKI such as SPRYCEL® (Dasatinib) and/or TASIGNA® (Nilotinib). All patients had prior treatment with GLEEVEC®, 85% had prior treatment with SPRYCEL® and 59% had prior treatment with TASGNA®. The primary end point was Major Cytogenetic Response (MCyR) and 81 patients with a median age of 59 years were included in this analysis. Treatment consisted of subcutaneous SYNRIBO®, administered at 1.25 mg/m2 twice daily for 14 consecutive days every 4 weeks until response, then for 7 days every 4 weeks as maintenance treatment. The median duration of treatment was 7.5 months. MCyR was noted in 20% of the patients and the median response duration was 17.7 months. Hematologic response was seen in 69% of the patients and the median response duration was 12.2 months. The median failure-free survival was 9.6 months and overall survival was 34 months. The most common grade 3/4 toxicities were cytopenias. The authors concluded that SYNRIBO® has clinical activity in a heavily pretreated population of patients with CML-CP and should therefore be considered for patients with CML-CP with resistance or intolerance to 2 or more TKI’s. By virtue of its mechanism of action, patients with T315I BCR-ABL mutation may potentially benefit from this unique compound. Cortes JE, Nicolini FE, Wetzler M, et al. Clin Lymphoma Myeloma Leuk. 2013;13:584-591.

PROSE: Randomized proteomic stratified phase III study of second line erlotinib versus chemotherapy in patients with inoperable non–small cell lung cancer (NSCLC)

SUMMARY: VeriStrat ® is a clinically validated serum/plasma-based assay, for patients with advanced Non Small Cell Lung Cancer (NSCLC). VeriStrat® is a serum test of prognostic and predictive value that classifies patients as VeriStrat-Good (VS-G) or VeriStrat-Poor (VS-P) based on eight mass spectral peaks or proteomic patterns of the patients serum. Proteomics is the large-scale study of protein structure and functions. VeriStrat® testing is protein based and therefore has no correlation with known genomic biomarkers. It is well established that EGFR-TKIs (Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitors) are more effective in NSCLC patients with EGFR activating mutations. PROSE is a multicenter, double blind, randomized, VeriStrat® stratified, phase III study. In this trial, over 90% of the patients had no EGFR mutations (EGFR-Wild Type). Two hundred and eighty five (285) patients with advanced NSCLC who had first line treatment regimen with platinum-based therapy were randomly assigned to receive second line chemotherapy (CT) with single agent ALIMTA® (Pemetrexed) or TAXOTERE® (Docetaxel), at standard doses (N=129) or TARCEVA® (Erlotinib) 150 mg po qd (N=134). Patients and study investigators were blinded to the patients VeriStrat® status. Patients were classified as VeriStrat-Good or VeriStrat-Poor based on the VeriStrat® results. Patients in the treatment groups were stratified by age, gender, tumor histology, ECOG-PS and smoking history. Crossover was permitted upon disease progression. The primary objective of the study was to demonstrate differential treatment benefit between TARCEVA® and CT with regards to Overall Survival (OS). Median overall survival (OS) was 9 months for the patients in the CT group and 7.7 months for TARCEVA® group and this was not statistically significant (P=0.3). However when evaluated by VeriStrat® status, CT was beneficial for the VeriStrat-Poor patients compared to TARCEVA®, with significantly better median OS (6.3 vs 3 months, P=0.02). Age, gender, histology (squamous vs non-squamous) and smoking history had no impact on the overall survival. The authors concluded that patients classified as VeriStrat-Poor have better survival with CT than TARCEVA®, whereas patients classified as VeriStrat-Good have similar survival with TARCEVA® and CT. VeriStrat® testing therefore, can help physicians choose between TARCEVA® and CT, for their patients with advanced NSCLC. This test helps physicians identify patients who are likely to have good or poor outcomes after treatment with EGFR inhibitors and thereby can provide valuable insight into whether CT or targeted therapy with TARCEVA®, a EGFR-TKI, is appropriate for their patients with advanced NSCLC, in the second line setting. This information is especially important for patients without an EGFR mutation or for those, whose EGFR mutation status is unknown. Sorlini C, Barni S, Petrelli F, et al. J Clin Oncol 29: 2011 (suppl; abstr TPS214)

 

PROSE Randomized proteomic stratified phase III study of second line erlotinib versus chemotherapy in patients with inoperable non–small cell lung cancer (NSCLC)

SUMMARY: VeriStrat ® is a clinically validated serum/plasma-based assay, for patients with advanced Non Small Cell Lung Cancer (NSCLC). VeriStrat® is a serum test of prognostic and predictive value that classifies patients as VeriStrat-Good (VS-G) or VeriStrat-Poor (VS-P) based on eight mass spectral peaks or proteomic patterns of the patients serum. Proteomics is the large-scale study of protein structure and functions. VeriStrat® testing is protein based and therefore has no correlation with known genomic biomarkers. It is well established that EGFR-TKIs (Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitors) are more effective in NSCLC patients with EGFR activating mutations. PROSE is a multicenter, double blind, randomized, VeriStrat® stratified, phase III study. In this trial, over 90% of the patients had no EGFR mutations (EGFR-Wild Type). Two hundred and eighty five (285) patients with advanced NSCLC who had first line treatment regimen with platinum-based therapy were randomly assigned to receive second line chemotherapy (CT) with single agent ALIMTA® (Pemetrexed) or TAXOTERE® (Docetaxel), at standard doses (N=129) or TARCEVA® (Erlotinib) 150 mg po qd (N=134). Patients and study investigators were blinded to the patients VeriStrat® status. Patients were classified as VeriStrat-Good or VeriStrat-Poor based on the VeriStrat® results. Patients in the treatment groups were stratified by age, gender, tumor histology, ECOG-PS and smoking history. Crossover was permitted upon disease progression. The primary objective of the study was to demonstrate differential treatment benefit between TARCEVA® and CT with regards to Overall Survival (OS). Median overall survival (OS) was 9 months for the patients in the CT group and 7.7 months for TARCEVA® group and this was not statistically significant (P=0.3). However when evaluated by VeriStrat® status, CT was beneficial for the VeriStrat-Poor patients compared to TARCEVA®, with significantly better median OS (6.3 vs 3 months, P=0.02). Age, gender, histology (squamous vs non-squamous) and smoking history had no impact on the overall survival. The authors concluded that patients classified as VeriStrat-Poor have better survival with CT than TARCEVA®, whereas patients classified as VeriStrat-Good have similar survival with TARCEVA® and CT. VeriStrat® testing therefore, can help physicians choose between TARCEVA® and CT, for their patients with advanced NSCLC. This test helps physicians identify patients who are likely to have good or poor outcomes after treatment with EGFR inhibitors and thereby can provide valuable insight into whether CT or targeted therapy with TARCEVA®, a EGFR-TKI, is appropriate for their patients with advanced NSCLC, in the second line setting. This information is especially important for patients without an EGFR mutation or for those, whose EGFR mutation status is unknown. Sorlini C, Barni S, Petrelli F, et al. J Clin Oncol 29: 2011 (suppl; abstr TPS214)

VERISTRAT® Testing – A novel approach to NSCLC

VeriStrat®, a serum based proteomic assay can help physicians identify patients who are likely to have good or poor outcomes after treatment with EGFR inhibitors and thereby can provide valuable insight into whether chemotherapy or targeted therapy with TARCEVA®, a EGFR-TKI, is appropriate for their patients with advanced NSCLC, in the second line setting. This information is especially important for patients without an EGFR mutation or for those, whose EGFR mutation status is unknown. In the PROSE trial, patients classified as VeriStrat-Poor have better survival with chemotherapy than TARCEVA®, whereas patients classified as VeriStrat-Good have similar survival with TARCEVA® and chemotherapy. This data was presented at the 2013 ASCO meeting.

Single-Agent Lenalidomide in Patients With Mantle-Cell Lymphoma Who Relapsed or Progressed After or Were Refractory to Bortezomib Phase II MCL-001 (EMERGE) Study

SUMMARY: In the MCL-001 trial, 134 patients with relapsed or refractory Mantle Cell Lymphoma (MCL) were enrolled. These patients had received prior treatment with RITUXAN® (Rituximab), CYTOXAN® (Cyclophosphamide), an Anthracycline and VELCADE® (Bortezomib) alone or in combination. The median age was 67 years and patients received a median of 4 prior therapies for MCL. Treatment consisted of Lenalidomide (REVLIMID®) 25 mg given orally on days 1 thru 21, of a 28 day cycle. Treatment was continued until disease progression or treatment intolerance. The primary efficacy endpoints were overall response rate (ORR) and duration of response (DOR). The secondary endpoints included Complete Response (CR), Progression Free Survival (PFS) and Overall Survival (OS). The ORR was 28% with a CR of 7% and the median DOR for those who responded to REVLIMID® was 16.6 months. The median PFS was 4 months and the median OS was 19 months.The most common grade 3-4 adverse reactions were cytopenias, fatigue, dyspnea and diarrhea. The authors concluded that REVLIMID® is the first drug to receive approval for the treatment of MCL since VELCADE® was approved for this disease in 2006 and gives one additional option for MCL patients, refractory to VELCADE®. Goy A, Sinha R, Williams ME, Besisik SK et al. J Clin Oncol 2013;31:3688-3695

Phase III Study of Afatinib or Cisplatin Plus Pemetrexed in Patients With Metastatic Lung Adenocarcinoma With EGFR Mutations

SUMMARY: GILOTRIF® (Afatinib) is an oral, irreversible blocker of the ErbB family which includes EGFR (ErbB1), HER2 (ErbB2), ErbB3 and ErbB4. The approval of GILOTRIF® was based on a multi-center, international, open-label, randomized, phase III trial, in which 345 patients with Stage IIIB (wet)/IV lung adenocarcinoma, with tumors demonstrating Epidermal Growth Factor Receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations, as detected by an FDA-approved test, were enrolled in a 2:1 ratio. Patients were randomized to receive GILOTRIF® 40 mg orally once daily (n=230) or ALIMTA® (Pemetrexed)/Cisplatin (n=115) given every 21 days for up to six cycles. Patients were stratified according to EGFR mutation status (exon 19 deletion vs. exon 21 L858R vs. ‘other’) and race (Asian vs. non-Asian). The primary endpoint was Progression Free Survival (PFS). The median PFS in the GILOTRIF® group was 11.1 months and 6.9 months in the chemotherapy group (HR= 0.58, P<0.001). In patients whose tumors demonstrated EGFR mutations, the median PFS was 13.6 months in the GILOTRIF® arm and 6.9 months in the chemotherapy arm (HR= 0.47, P<0.001). Objective response rates were 56% and 23% in the GILOTRIF® and chemotherapy groups respectively (P=0.001). There was no statistically significant difference in overall survival between the two treatment groups. The most frequent adverse reactions in the GILOTRIF® group were skin rash, pruritus, stomatitis, diarrhea and decreased appetite. The authors concluded that GILOTRIF® is better than chemotherapy in the first line treatment of EGFR mutant Non Small Cell Lung Cancer patients. However, it remains to be seen if this agent is superior to TARCEVA® (Erlotinib) and IRESSA® (Gefitinib). Sequist LV, Yang JC, Yamamoto N, et al. J Clin Oncol 2013;31:3327-3334