Archive for the ‘Chemotherapeutic / Anti-Neoplastic’ Category

Progression Free Survival Goal Met With Cobimetinib

Monday, August 11th, 2014

Vemurafenib and Cobimetinib- a Dynamic Duo in the Fight Against MelanomaImpressive news was revealed from Roche and Exelixis on June 14, 2014 with successful Phase III study results from their melanoma trial. This comprehensive trial involved Exelixis’s Cobimetinib and Zelboraf, which is marketed by Roche, for treating patients with advanced cases of melanoma. All of the 495 patients had specific mutations of the BRAF gene and many were considered to have unresectable cases of this deadly skin cancer. The surprise for clinical trial investigators came when they found the concomitant use of these two drugs led to a longer progression free survival for patients in comparison to their treatment with Zelboraf alone. These top line results are exciting for the medical and pharmaceutical community as this data clears the way for an upcoming FDA application. The Phase III study, coined coBRIM not only met its primary goal of progression free survival, thanks to the addition of Cobimetinib, but it also proved to be safe and tolerable.

Cobimetinib is a highly selective inhibitor of mitogen-activated protein kinase MEK, and has demonstrated efficacious ability sustain the inhibition of MEK in both mutant RAS and BRAF tumor models. The development of Cobimetinib is currently under Roche and Genentech, with a collaboration agreement with Exelixis. A successful Phase 1b dose escalation study of Cobimetinib, called BRIM7, proved this potent drug was effectual when used adjunctively with the BRAF inhibitor Vemurafenib. The BRIM7 study involved patients with metastatic cases of melanoma who had the BRAFV600 mutation, with the results being presented at the 10th European Association of Dermato-Oncology Congress in May 2014.

Clinical trials are ongoing for Cobimetinib alongside other anti-cancer agents, and many of the patients accepted in these trials are chosen specifically for their genetic mutations. Current studies include combining Cobimetinib with: GDC-0068, an AKT inhibitor; Onartuzumab, a MET targeting antibody; MEHD7945A, a biotherapeutic targeting EGFR and HER3; and GDC-0941, a PI3K inhibitor. This patient population is facing a critical need for new and innovative treatment, and Cobimetinib looks like it may be the agent to meet this need.

LGM Pharma is a provider of the API Cobimetinib, CAS # 934660-93-2 for research and development purposes. Clients can be assured of quality API products and continuous support throughout the R&D process.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

 

Tipiracil and Trifluridine Are Powerful Opponents Against Colorectal Cancer

Thursday, July 31st, 2014

Tipiracil and Trifluridine Are Powerful Opponents Against Colorectal CancerPositive findings were recently revealed from Taiho Oncology Inc. with the revelation of their global Phase 3 trial coined RECOURSE. This extensive trial was of the anticancer combination duo Tipiracil and Trifluridine, also called TAS-102. Data disseminated from this Phase 3 trial demonstrated that TAS-102 reduced the risk of mortality for patients with unresectable colon cancer by 32 percent as compared to a placebo. Clinical trial participants also achieved statistically sizable improvements in progression free and overall survival, including patients who were previously intolerant to former therapies. This inspiring data was presented at the European Society for Medical Oncology 16th World Congress on Gastrointestinal Cancer, which was held in Barcelona, Spain.

The RECOURSE trial included 800 patients that were randomized to receive best in care treatments either with or without the formidable TAS-102 combination treatment. All of the patients enrolled in this Phase 3 trial had completed on average two previous therapies which were deemed unsuccessful. Both the primary outcome measure of increased overall survival and secondary endpoint of progression-free survival were met.

The patient group who were administered Tipiracil and Trifluridine { TAS-102} gained an overall survival time of 7.1 months, as well as a 52 percent decrease in the risk of disease progression as compared to the placebo arm of the study. Clinically relevant results from the dynamic duo Tipiracil and Trifluridine clearly offered patients with refractory metastatic colon cancer a viable chance at extended survival. As efficacious antitumor agents both Tipiracil and Trifluridine have proven tolerable for and safe for patients in studies. Adverse effects were reported, but there were no participants who withdrew due to these effects. Most commonly reported side effects included diarrhea, anemia, leukopenia, vomiting, nausea, neutropenia and fatigue.

Colorectal Cancer Statistics

Colorectal cancer is the third most common cancer for American men and women. The American Cancer Society offers daunting statistics estimating that the lifetime risk of developing this potentially fatal disease is 1 in 20 people in the U.S. Approximately 96,830 new cases of colon cancer are diagnosed each year in the United States, along with roughly 40,000 new cases of rectal cancer. Estimates regarding the mortality of patients diagnosed with colon cancer are of great concern as well, with an estimated 50,310 fatalities predicted in 2014. Novel treatments which improve overall survival and extend progression free survival are critically necessary.

LGM Pharma is a provider of Trifluridine, CAS# 70-00-8, and Tipiracil, CAS# 183204-74-2 APIs for research and development purposes. Clients can be assured of quality API products and continuous support throughout the R&D process.

 

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

Idelalisib FDA Approved to Combat Three Blood Cancers

Monday, July 28th, 2014

Idelalisib is FDA Approved Gilead has announced the July 23, 2014 Idelalisib FDA approved news. The Idelalisib (or the brand name Zydelig) approval was long awaited, to combat three forms of blood cancer. The FDA extended a nod to this powerful drug, which is estimated to earn roughly 1.2 billion dollars by the year 2020. Approved to treat three type of B-cell blood cancer, Idelalisib is effective for relapsed follicular B-cell non-Hodgkin lymphoma, relapsed chronic lymphocytic leukemia and small lymphocytic lymphoma. As a formidable first-in-class PI3k inhibitor Idelalisib will be administered along with Rituximab for patients fighting refractory chronic lymphocytic leukemia. While there is a slight risk of serious toxicities, the majority of patients had common adverse reactions that were not deemed severe, and included pyrexia, abdominal pain, diarrhea, nausea and a mild rash. These adverse effects were seen in patients who were administered Idelalisib both with and without the addition of Rituximab.

Phase III results were impressive for Zydelig {Idelalisib}, showing a response rate of 81 percent. When clinical study participants received both Idelalisib and Rituximab to treat refractory chronic lymphocytic leukemia patients gleaned a 93 percent progression-free survival rate at 24 weeks. The advent of Idelalisib offers patients with these hard to treat forms of blood cancers better options for treatment and hope for tangible progression free survival. Idelalisib is also easy to administer as oral tablets which are typically taken twice daily, either with or without food. There are over 200,000 patients in the United States who suffer from relapsed follicular B-cell non-Hodgkin lymphoma, relapsed chronic lymphocytic leukemia or small lymphocytic lymphoma. This patient population is clearly in need of innovative and effective treatments.

LGM Pharma can assist clients as a provider of Idelalisib, CAS # 870281-82-6, for research and development purposes. Clients can be assured of quality API products and continuous support throughout the R&D process.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

 

 

Anti- Cancer Drug Volasertib Achieves Exemplary Results in Phase II Study

Monday, July 21st, 2014

volasertibBoehringer Ingelheim recently shared exciting Phase II results from their anti-cancer breakthrough drug Volasertib. Patients enrolled in this landmark study, revealed July 8, 2014, had acute myeloid leukemia, or AML, and were considered to have unresectable cases. The study encompassed an elderly patient population, with every participant being over the age of 65. Results have been declared unusually positive, with survival rates rivaling similar midstage study results of standard chemotherapy. Patients with AML who received a combination of Volasertib and low dose chemotherapy experienced a median overall survival rate of 8 months, in comparison to the patients who were dosed with standard best in care chemotherapy alone. The patients who were administered chemotherapy without Volasertib had a median overall survival rate of 5.2 months. Additionally, the event-free survival rate was 5.6 months for the patient arm who were given both Volasertib and chemotherapy, over twice as long as the rate of patients who were dosed with chemotherapy only, which was 2.3 months of event free survival.

Volasertib is an effective inhibitor of the polo-like kinase which in turn spurs cancer cell death. Acute myeloid leukemia typically affects the elderly population, so Phase II study results of this formidable drug are encouraging, especially for patients who cannot tolerate large amounts of chemotherapy as their only treatment option. A Phase III study of Volasertib is currently underway, with 660 patients suffering from acute myeloid leukemia. The Phase III study will be a multicenter, double-blind trial which is on target to conclude in 2016.

On April 17, 2014 Volasertib was granted Orphan Drug Designation for acute myeloid leukemia by both the European Commission and the FDA. This designation offered hope to the patients inflicted with AML, which is a rare but aggressive type of bone marrow and blood cancer. This virulent disease primarily affects people over the age of 60 and is the cause of approximately one third of adult leukemias in the Western World. Volasertib offers a treatment option for patients with AML who cannot tolerate standard chemotherapy or need the adjunctive use of another anti-cancer agent.

LGM Pharma is a provider of Volasertib, CAS # 755038-65-4, for research and development purposes. Clients can be assured of quality API products and continuous support throughout the R&D process.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

Mocetinostat Receives Orphan Drug Designation

Monday, July 14th, 2014

Mocetinostat Receives Orphan Drug Designation

Exciting news was revealed on June 18, 2014 with the announcement that Mocetinostat garnished an Orphan Drug Designation from the FDA. Information gleaned from a Phase 1/2 study of Mocetinostat showed that when used alongside Azacitidine (Vidaza) this combination provided efficacious treatment for patients with myelodysplastic syndromes. Patients who were at intermediate or high risk myelodysplastic syndromes, also known as MDS demonstrated a high response rate to this dynamic duo. Roughly 64 percent of patients with MDS who were administered both Azacitidine and Mocetinostat showed a viable response to the treatment, and a startling 50 percent of patients achieved a complete response. Addtionally, 33 percent of patients gained transfusion independence after their treatment regimen with Azacitidine and Mocetinostat. Although Vidaza (Azacitidine) has been proven effective independently of Mocetinostat, the addition of this drug has offered a sizable increase in response rate, particularly in high risk MDS patients. A Phase I trial is currently underway to determine the safety, tolerability and efficacy of Mocetinostat and Azacitidine, although the planned dosage of Mocetinostat will be slightly lower in than was administered during the 1/2 trial phase.

hematopoieticStudy results from 22 patients with MDS made up the data for the 1/2 trial of Azacitidine and Mocetinostat. These patients were considered as intermediate and high risk, as they possessed either refractory anemia with excess blasts-1 (RAEB-1) or RAEB-2. The average age of the clinical trial participants was 72 years old, with 64 percent of the patients having blast counts between 10 and 20 percent. The majority of patients had received no previous first line therapy, while a little over 40 percent of the participants had received therapy but not with Azacitidine or Mocetinostat. When the ½ trial commenced patients were administered 75 mg/m2 of Azacitidine subcutaneously. This protocol lasted for the first seven days of a 28-day cycle of treatment. Roughly 80 percent of the participants were dosed with 90 milligrams of Mocetinostat three times per week during the 28 day cycle, beginning on the fifth day of treatment with Azacitidine. The remaining 20 percent of patients received a 110 milligram or 135 milligram dose of Mocetinostat on the same schedule. After 4.5 cycles of treatment positive results emerged, with half of all participants achieving a complete response. Additionally, 5 percent of people displayed improvements in their blood cell counts. Low platelet counts, diarrhea and fatigue dominated the side effects, however no catastrophic adverse events occurred. Over 447 patients in 13 clinical trials have received treatment with Mocetinostat, which have overall been encouraging. There are 28 patients documented to have achieved a 93 percent disease control rate thus far, and the number is expected to increase as continued research and development plays out.

As a histone deacetylase inhibitor Mocetinostat works by raising the production of proteins in the body which cause cell death and slow cell division. Myelodysplastic syndromes are cancerous conditions that typically occur when the blood-forming cells in the bone marrow become damaged. The unfortunate damage leads to lower numbers of one or several types of blood cells, and many of the blood cells formed by the damaged bone marrow cells are ultimately considered defective. About one-third of patients see their diagnosis of MDS progress quickly to acute myeloid leukemia. Research and development of new and effectual treatments to combat myelodysplastic syndromes is urgent.

LGM Pharma is a provider of the APIs Azacitidine (TEVA API) CAS # 320-67-2 and Mocetinostat CAS# 726169-73-9 for research and development purposes. Clients can be assured of quality API products and continuous support throughout the R&D process.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.