Bristol-Myers Squibb’s Opdivo® (nivolumab) + Low-Dose Yervoy® (ipilimumab) is the First Immuno-Oncology Combination Approved for MSI-H/dMMR mCRC Patients Who Progressed Following Treatment with a Fluoropyrimidine, Oxaliplatin and…

On July 11, 2018 Bristol-Myers Squibb Company (NYSE: BMY) reported Opdivo (nivolumab) 3 mg/kg plus low-dose Yervoy (ipilimumab) 1 mg/kg (injections for intravenous use) received approval from the U.S. Food and Drug Administration (FDA) for the treatment of adult and pediatric patients 12 years and older with microsatellite instability high (MSI-H) or mismatch repair deficient (dMMR) metastatic colorectal cancer (mCRC) that has progressed following treatment with a fluoropyrimidine, oxaliplatin and irinotecan (Press release, Bristol-Myers Squibb, JUL 11, 2018, View Source [SID1234527642]).1 Approval for this indication has been granted under accelerated approval based on overall response rate (ORR) and duration of response (DOR).1 Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.

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"Bristol-Myers Squibb is pleased to bring forward Opdivo plus Yervoy as the first I-O/I-O combination therapy to be approved in this type of colorectal cancer," said Ian M. Waxman, M.D., development lead, gastrointestinal cancers, Bristol-Myers Squibb. "Our commitment to studying Opdivo plus Yervoy, which target distinct but complementary immune pathways, results from our strong belief that rational combinations in biomarker-selected populations may improve clinical benefit for patients."

Opdivo + Yervoy is associated with the following Warnings and Precautions: immune-mediated pneumonitis, colitis, hepatitis, endocrinopathies, nephritis and renal dysfunction, skin adverse reactions, encephalitis, other adverse reactions; infusion reactions; and embryo-fetal toxicity. Please see the Important Safety Information section below, including Boxed WARNING for Yervoy regarding immune-mediated adverse reactions, as well as additional information on CheckMate -142.1,2

Today’s approved indication was based on data from the ongoing Phase 2 CheckMate -142 study evaluating the Opdivo + Yervoy combination in patients with MSI-H or dMMR mCRC previously treated with a fluoropyrimidine-, oxaliplatin- or irinotecan-based chemotherapy.1,3,4 The application was granted Priority Review and Breakthrough Therapy Designation by the FDA.

The Opdivo + Yervoy cohort of the CheckMate -142 trial enrolled MSI-H/dMMR mCRC patients who had received at least one prior line of therapy for metastatic disease, and efficacy was analyzed for both patients who had received prior treatment with a fluoropyrimidine, oxaliplatin and irinotecan (82 of the total 119 patients) as well as for all enrolled patients.1

Among the 82 patients who received prior treatment with a fluoropyrimidine, oxaliplatin and irinotecan, 46% (95% CI: 35-58; n = 38/82) responded to treatment with Opdivo + Yervoy as assessed by Independent Radiographic Review Committee (IRRC).1
The percentage of these patients with a complete response was 3.7% (n = 3/82), and the percentage of patients with a partial response was 43% (n = 35/82).1 Among these 38 responders, the median DOR was not reached (range: 1.9-23.2+ months); 89% of those patients had responses of six months or longer, and 21% had responses of 12 months or longer.1,5,6 This trial is ongoing.3
Among all enrolled patients, 49% (95% CI: 39-58; n = 58/119) responded to treatment with Opdivo + Yervoy; 4.2% (n = 5/119) experienced a complete response, while 45% (n = 53/119) experienced a partial response.1 Among these 58 responders, the median DOR was not reached (range: 1.9-23.2+ months)5,6; 83% of those patients had responses of six months or longer, and 19% had responses of 12 months or longer.1 In the combination cohort, 51 of 58 responders were ongoing at the time of database lock; 78% of these ongoing responders had not reached 12 months of follow-up from the date of onset of response.1
The recommended dosing schedule includes the Opdivo + low-dose Yervoy combination (Opdivo 3 mg/kg, administered as an I.V. infusion over 30 minutes, followed by Yervoy 1 mg/kg, administered as an I.V. infusion over 30 minutes, on the same day, every three weeks for four doses), followed by Opdivo maintenance therapy (240 mg, administered as an I.V. infusion over 30 minutes, every two weeks) after completion of four doses of the combination until disease progression or unacceptable toxicity.1 Please review the U.S. Full Prescribing Information for Yervoy prior to initiation.

In the Opdivo + Yervoy cohort of CheckMate -142, 86% of patients received all four doses of Opdivo + Yervoy.7 Opdivo was discontinued in 13% of patients and delayed in 45% of patients due to an adverse reaction.1 Serious adverse reactions occurred in 47% of patients.1

"Metastatic colorectal cancers with dMMR or MSI-H biomarkers can be difficult to treat and some patients may need additional options," said Heinz-Josef Lenz, M.D., FACP, L. Terrence Lanni Chair in Gastrointestinal Cancer Research, Keck School of Medicine of University of Southern California and principal investigator of the study at USC Norris Comprehensive Cancer Center. "The FDA’s approval of an I-O/I-O combination provides us with an encouraging approach to address this challenging disease in patients who have progressed following treatment with three standard chemotherapy options."

The Opdivo + Yervoy combination is also approved in two other tumor types. The Opdivo (3 mg/kg) + low-dose Yervoy (1 mg/kg) combination is approved for previously untreated patients with intermediate- or poor-risk advanced renal cell carcinoma. Opdivo (1 mg/kg) + Yervoy (3 mg/kg) is approved for patients with unresectable or metastatic melanoma under accelerated approval based on progression-free survival. Opdivo as a single agent is approved for the treatment of adult and pediatric (12 years and older) patients with MSI-H or dMMR metastatic colorectal cancer that has progressed following treatment with a fluoropyrimidine, oxaliplatin and irinotecan under accelerated approval based on ORR and DOR. Continued approval for these accelerated approval indications may be contingent upon verification and description of clinical benefit in the confirmatory trials. The infusion time for each indication differs, please see U.S. Full Prescribing Information for Opdivo and Yervoy for details.1

Approval Based on CheckMate -142 Trial

CheckMate -142 included a multicenter, non-randomized, multiple-parallel cohort, open-label study investigating Opdivo + Yervoy in patients with locally determined dMMR or MSI-H mCRC whose disease had progressed during or after prior treatment with a fluoropyrimidine-, oxaliplatin- or irinotecan-based chemotherapy.1,8 In the combination cohort, patients received Opdivo 3 mg/kg with Yervoy 1 mg/kg every three weeks for four doses, followed by Opdivo 3 mg/kg as a single agent every two weeks.1 Treatment continued until unacceptable toxicity or radiographic progression.1 Tumor assessments were conducted every six weeks for the first 24 weeks and every 12 weeks thereafter.1 Efficacy outcome measures included ORR as assessed by IRRC using Response Evaluation Criteria in Solid Tumors (RECIST v1.1) and DOR.1 Data from this study were presented in January at the 2018 Gastrointestinal Cancers Symposium and published simultaneously in the Journal of Clinical Oncology.

Select Safety Profile for the CheckMate -142 Trial

The most frequent serious adverse reactions reported in at least 2% of patients were colitis/diarrhea, hepatic events, abdominal pain, acute kidney injury, pyrexia, and dehydration.1 The most common adverse reactions (reported in at least 20% of patients) were fatigue (49%), diarrhea (45%), pyrexia (36%), musculoskeletal pain (36%), abdominal pain (30%), pruritus (28%), nausea (26%), rash (25%), decreased appetite (20%), and vomiting (20%).1

About MSI-H or dMMR Colorectal Cancer

Colorectal cancer (CRC) is cancer that develops in the colon or the rectum, which are part of the body’s digestive or gastrointestinal system.10 In the United States, CRC is the third most common cancer.10 In 2018, it is estimated that there will be approximately 140,000 new cases of the disease and that it will be the third leading cause of cancer-related deaths among men and women combined.10

DNA mismatch repair deficiency (dMMR) occurs when the proteins that repair mismatch errors in DNA replication are missing or non-functional, leading to microsatellite instability-high (MSI-H) tumors.11,12 Approximately 5% of metastatic CRC patients have dMMR or MSI-H tumors.13 Patients with these biomarkers are less likely to benefit from conventional chemotherapy and typically have a poor prognosis.11,13,14

INDICATIONS

OPDIVO (nivolumab), in combination with YERVOY (ipilimumab), is indicated for the treatment of patients with unresectable or metastatic melanoma. This indication is approved under accelerated approval based on progression-free survival. Continued approval for this indication may be contingent upon verification and description of clinical benefit in the confirmatory trials.

OPDIVO (nivolumab), in combination with YERVOY (ipilimumab), is indicated for the treatment of patients with intermediate or poor risk, previously untreated advanced renal cell carcinoma (RCC).

OPDIVO (nivolumab), as a single agent, is indicated for the treatment of adult and pediatric (12 years and older) patients with microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR) metastatic colorectal cancer (CRC) that has progressed following treatment with a fluoropyrimidine, oxaliplatin, and irinotecan. This indication is approved under accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.

OPDIVO (nivolumab), in combination with YERVOY (ipilimumab), is indicated for the treatment of adults and pediatric patients 12 years and older with microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR) metastatic colorectal cancer (CRC) that has progressed following treatment with a fluoropyrimidine, oxaliplatin, and irinotecan. This indication is approved under accelerated approved based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.

OPDIVO (10 mg/mL) and YERVOY (5 mg/mL) are injections for intravenous use.

IMPORTANT SAFETY INFORMATION

WARNING: IMMUNE-MEDIATED ADVERSE REACTIONS

YERVOY can result in severe and fatal immune-mediated adverse reactions. These immune-mediated reactions may involve any organ system; however, the most common severe immune-mediated adverse reactions are enterocolitis, hepatitis, dermatitis (including toxic epidermal necrolysis), neuropathy, and endocrinopathy. The majority of these immune-mediated reactions initially manifested during treatment; however, a minority occurred weeks to months after discontinuation of YERVOY.

Assess patients for signs and symptoms of enterocolitis, dermatitis, neuropathy, and endocrinopathy, and evaluate clinical chemistries including liver function tests (LFTs), adrenocorticotropic hormone (ACTH) level, and thyroid function tests, at baseline and before each dose.

Permanently discontinue YERVOY and initiate systemic high-dose corticosteroid therapy for severe immune-mediated reactions.

Immune-Mediated Pneumonitis

OPDIVO can cause immune-mediated pneumonitis. Fatal cases have been reported. Monitor patients for signs with radiographic imaging and for symptoms of pneumonitis. Administer corticosteroids for Grade 2 or more severe pneumonitis. Permanently discontinue for Grade 3 or 4 and withhold until resolution for Grade 2. In patients receiving OPDIVO monotherapy, fatal cases of immune-mediated pneumonitis have occurred. Immune-mediated pneumonitis occurred in 3.1% (61/1994) of patients. In patients receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg, immune-mediated pneumonitis occurred in 6% (25/407) of patients. In RCC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated pneumonitis occurred in 4.4% (24/547) of patients. In MSI-H/dMMR mCRC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated pneumonitis occurred in 1.7% (2/119) of patients.

Immune-Mediated Colitis

OPDIVO can cause immune-mediated colitis. Monitor patients for signs and symptoms of colitis. Administer corticosteroids for Grade 2 (of more than 5 days duration), 3, or 4 colitis. Withhold OPDIVO monotherapy for Grade 2 or 3 and permanently discontinue for Grade 4 or recurrent colitis upon re-initiation of OPDIVO. When administered with YERVOY, withhold OPDIVO and YERVOY for Grade 2 and permanently discontinue for Grade 3 or 4 or recurrent colitis. In patients receiving OPDIVO monotherapy, immune-mediated colitis occurred in 2.9% (58/1994) of patients. In patients receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg, immune-mediated colitis occurred in 26% (107/407) of patients including three fatal cases. In RCC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated colitis occurred in 10% (52/547) of patients. In MSI-H/dMMR mCRC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated colitis occurred in 7% (8/119) of patients.

In a separate Phase 3 study of YERVOY 3 mg/kg, severe, life-threatening, or fatal (diarrhea of ≥7 stools above baseline, fever, ileus, peritoneal signs; Grade 3-5) immune-mediated enterocolitis occurred in 34 (7%) patients. Across all YERVOY-treated patients in that study (n=511), 5 (1%) developed intestinal perforation, 4 (0.8%) died as a result of complications, and 26 (5%) were hospitalized for severe enterocolitis.

Immune-Mediated Hepatitis

OPDIVO can cause immune-mediated hepatitis. Monitor patients for abnormal liver tests prior to and periodically during treatment. Administer corticosteroids for Grade 2 or greater transaminase elevations. Withhold OPDIVO for Grade 2 and permanently discontinue OPDIVO for Grade 3 or 4. In patients receiving OPDIVO monotherapy, immune-mediated hepatitis occurred in 1.8% (35/1994) of patients. In patients receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg, immune-mediated hepatitis occurred in 13% (51/407) of patients. In RCC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated hepatitis occurred in 7% (38/547) of patients. In MSI-H/dMMR mCRC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated hepatitis occurred in 8% (10/119) of patients.

In a separate Phase 3 study of YERVOY 3 mg/kg, severe, life-threatening, or fatal hepatotoxicity (AST or ALT elevations >5x the ULN or total bilirubin elevations >3x the ULN; Grade 3-5) occurred in 8 (2%) patients, with fatal hepatic failure in 0.2% and hospitalization in 0.4%.

Immune-Mediated Neuropathies

In a separate Phase 3 study of YERVOY 3 mg/kg, 1 case of fatal Guillain-Barré syndrome and 1 case of severe (Grade 3) peripheral motor neuropathy were reported.

Immune-Mediated Endocrinopathies

OPDIVO can cause immune-mediated hypophysitis, immune-mediated adrenal insufficiency, autoimmune thyroid disorders, and Type 1 diabetes mellitus. Monitor patients for signs and symptoms of hypophysitis, signs and symptoms of adrenal insufficiency, thyroid function prior to and periodically during treatment, and hyperglycemia. Administer hormone replacement as clinically indicated and corticosteroids for Grade 2 or greater hypophysitis. Withhold for Grade 2 or 3 and permanently discontinue for Grade 4 hypophysitis. Administer corticosteroids for Grade 3 or 4 adrenal insufficiency. Withhold for Grade 2 and permanently discontinue for Grade 3 or 4 adrenal insufficiency. Administer hormone-replacement therapy for hypothyroidism. Initiate medical management for control of hyperthyroidism. Withhold OPDIVO for Grade 3 and permanently discontinue for Grade 4 hyperglycemia.

In patients receiving OPDIVO monotherapy, hypophysitis occurred in 0.6% (12/1994) of patients. In patients receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg, hypophysitis occurred in 9% (36/407) of patients. In RCC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, hypophysitis occurred in 4.6% (25/547) of patients. In MSI-H/dMMR mCRC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated hypophysitis occurred in 3.4% (4/119) of patients. In patients receiving OPDIVO monotherapy, adrenal insufficiency occurred in 1% (20/1994) of patients. In patients receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg, adrenal insufficiency occurred in 5% (21/407) of patients. In RCC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, adrenal insufficiency occurred in 7% (41/547) of patients. In MSI-H/dMMR mCRC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, adrenal insufficiency occurred in 5.9% (7/119) of patients. In patients receiving OPDIVO monotherapy, hypothyroidism or thyroiditis resulting in hypothyroidism occurred in 9% (171/1994) of patients. Hyperthyroidism occurred in 2.7% (54/1994) of patients receiving OPDIVO monotherapy. In patients receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg, hypothyroidism or thyroiditis resulting in hypothyroidism occurred in 22% (89/407) of patients. Hyperthyroidism occurred in 8% (34/407) of patients receiving this dose of OPDIVO with YERVOY. In RCC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, hypothyroidism or thyroiditis resulting in hypothyroidism occurred in 22% (119/547) of patients. Hyperthyroidism occurred in 12% (66/547) of patients receiving this dose of OPDIVO with YERVOY. In MSI-H/dMMR mCRC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, hypothyroidism or thyroiditis resulting in hypothyroidism occurred in 15% (18/119) of patients. Hyperthyroidism occurred in 12% (14/119) of patients. In patients receiving OPDIVO monotherapy, diabetes occurred in 0.9% (17/1994) of patients. In patients receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg, diabetes occurred in 1.5% (6/407) of patients. In RCC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, diabetes occurred in 2.7% (15/547) of patients.

In a separate Phase 3 study of YERVOY 3 mg/kg, severe to life-threatening immune-mediated endocrinopathies (requiring hospitalization, urgent medical intervention, or interfering with activities of daily living; Grade 3-4) occurred in 9 (1.8%) patients. All 9 patients had hypopituitarism, and some had additional concomitant endocrinopathies such as adrenal insufficiency, hypogonadism, and hypothyroidism. Six of the 9 patients were hospitalized for severe endocrinopathies.

Immune-Mediated Nephritis and Renal Dysfunction

OPDIVO can cause immune-mediated nephritis. Monitor patients for elevated serum creatinine prior to and periodically during treatment. Administer corticosteroids for Grades 2-4 increased serum creatinine. Withhold OPDIVO for Grade 2 or 3 and permanently discontinue for Grade 4 increased serum creatinine. In patients receiving OPDIVO monotherapy, immune-mediated nephritis and renal dysfunction occurred in 1.2% (23/1994) of patients. In patients receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg, immune-mediated nephritis and renal dysfunction occurred in 2.2% (9/407) of patients. In RCC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated nephritis and renal dysfunction occurred in 4.6% (25/547) of patients. In MSI-H/dMMR mCRC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated nephritis and renal dysfunction occurred in 1.7% (2/119) of patients.

Immune-Mediated Skin Adverse Reactions and Dermatitis

OPDIVO can cause immune-mediated rash, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), some cases with fatal outcome. Administer corticosteroids for Grade 3 or 4 rash. Withhold for Grade 3 and permanently discontinue for Grade 4 rash. For symptoms or signs of SJS or TEN, withhold OPDIVO and refer the patient for specialized care for assessment and treatment; if confirmed, permanently discontinue. In patients receiving OPDIVO monotherapy, immune-mediated rash occurred in 9% (171/1994) of patients. In patients receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg, immune-mediated rash occurred in 22.6% (92/407) of patients. In RCC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated rash occurred in 16.6% (91/547) of patients. In MSI-H/dMMR mCRC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, immune-mediated rash occurred in 14% (17/119) of patients.

In a separate Phase 3 study of YERVOY 3 mg/kg, severe, life-threatening, or fatal immune-mediated dermatitis (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis, or rash complicated by full thickness dermal ulceration, or necrotic, bullous, or hemorrhagic manifestations; Grade 3-5) occurred in 13 (2.5%) patients. 1 (0.2%) patient died as a result of toxic epidermal necrolysis. 1 additional patient required hospitalization for severe dermatitis.

Immune-Mediated Encephalitis

OPDIVO can cause immune-mediated encephalitis. Evaluation of patients with neurologic symptoms may include, but not be limited to, consultation with a neurologist, brain MRI, and lumbar puncture. Withhold OPDIVO in patients with new-onset moderate to severe neurologic signs or symptoms and evaluate to rule out other causes. If other etiologies are ruled out, administer corticosteroids and permanently discontinue OPDIVO for immune-mediated encephalitis. In patients receiving OPDIVO monotherapy, encephalitis occurred in 0.2% (3/1994) of patients. Fatal limbic encephalitis occurred in one patient after 7.2 months of exposure despite discontinuation of OPDIVO and administration of corticosteroids. Encephalitis occurred in one patient receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg (0.2%) after 1.7 months of exposure. Encephalitis occurred in one RCC patient receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg (0.2%) after approximately 4 months of exposure. Encephalitis occurred in one MSI-H/dMMR mCRC patient (0.8%) receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg after 15 days of exposure.

Other Immune-Mediated Adverse Reactions

Based on the severity of the adverse reaction, permanently discontinue or withhold OPDIVO, administer high-dose corticosteroids, and if appropriate, initiate hormone-replacement therapy. Across clinical trials of OPDIVO monotherapy or in combination with YERVOY, the following clinically significant immune-mediated adverse reactions, some with fatal outcome, occurred in <1.0% of patients receiving OPDIVO: myocarditis, rhabdomyolysis, myositis, uveitis, iritis, pancreatitis, facial and abducens nerve paresis, demyelination, polymyalgia rheumatica, autoimmune neuropathy, Guillain-Barré syndrome, hypopituitarism, systemic inflammatory response syndrome, gastritis, duodenitis, sarcoidosis, histiocytic necrotizing lymphadenitis (Kikuchi lymphadenitis), motor dysfunction, vasculitis, aplastic anemia, pericarditis, and myasthenic syndrome.

If uveitis occurs in combination with other immune-mediated adverse reactions, consider a Vogt-Koyanagi-Harada-like syndrome, which has been observed in patients receiving OPDIVO and may require treatment with systemic steroids to reduce the risk of permanent vision loss.

Infusion Reactions

OPDIVO can cause severe infusion reactions, which have been reported in <1.0% of patients in clinical trials. Discontinue OPDIVO in patients with Grade 3 or 4 infusion reactions. Interrupt or slow the rate of infusion in patients with Grade 1 or 2. In patients receiving OPDIVO monotherapy as a 60-minute infusion, infusion-related reactions occurred in 6.4% (127/1994) of patients. In a separate study in which patients received OPDIVO monotherapy as a 60-minute infusion or a 30-minute infusion, infusion-related reactions occurred in 2.2% (8/368) and 2.7% (10/369) of patients, respectively. Additionally, 0.5% (2/368) and 1.4% (5/369) of patients, respectively, experienced adverse reactions within 48 hours of infusion that led to dose delay, permanent discontinuation or withholding of OPDIVO. In patients receiving OPDIVO 1 mg/kg with YERVOY 3 mg/kg every 3 weeks, infusion-related reactions occurred in 2.5% (10/407) of patients. In RCC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, infusion-related reactions occurred in 5.1% (28/547) of patients. In MSI-H/dMMR mCRC patients receiving OPDIVO 3 mg/kg with YERVOY 1 mg/kg, infusion-related reactions occurred in 4.2% (5/119) of patients.

Embryo-Fetal Toxicity

Based on their mechanisms of action, OPDIVO and YERVOY 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 an OPDIVO- or YERVOY- containing regimen and for at least 5 months after the last dose of OPDIVO.

Lactation

It is not known whether OPDIVO or YERVOY is present in human milk. Because many drugs, including antibodies, are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from an OPDIVO-containing regimen, advise women to discontinue breastfeeding during treatment. Advise women to discontinue breastfeeding during treatment with YERVOY and for 3 months following the final dose.

Serious Adverse Reactions

In Checkmate 067, serious adverse reactions (73% and 37%), adverse reactions leading to permanent discontinuation (43% and 14%) or to dosing delays (55% and 28%), and Grade 3 or 4 adverse reactions (72% and 44%) all occurred more frequently in the OPDIVO plus YERVOY arm (n=313) relative to the OPDIVO arm (n=313). The most frequent (≥10%) serious adverse reactions in the OPDIVO plus YERVOY arm and the OPDIVO arm, respectively, were diarrhea (13% and 2.6%), colitis (10% and 1.6%), and pyrexia (10% and 0.6%). In Checkmate 214, serious adverse reactions occurred in 59% of patients receiving OPDIVO plus YERVOY and in 43% of patients receiving sunitinib. The most frequent serious adverse reactions reported in ≥2% of patients were diarrhea, pyrexia, pneumonia, pneumonitis, hypophysitis, acute kidney injury, dyspnea, adrenal insufficiency, and colitis; in patients treated with sunitinib, they were pneumonia, pleural effusion, and dyspnea. In Checkmate 142 in MSI-H/dMMR mCRC patients receiving OPDIVO with YERVOY, serious adverse reactions occurred in 47% of patients. The most frequent serious adverse reactions reported in ≥2% of patients were colitis/diarrhea, hepatic events, abdominal pain, acute kidney injury, pyrexia, and dehydration.

Common Adverse Reactions

In Checkmate 067, the most common (≥20%) adverse reactions in the OPDIVO plus YERVOY arm (n=313) were fatigue (59%), rash (53%), diarrhea (52%), nausea (40%), pyrexia (37%), vomiting (28%), and dyspnea (20%). The most common (≥20%) adverse reactions in the OPDIVO (n=313) arm were fatigue (53%), rash (40%), diarrhea (31%), and nausea (28%). In Checkmate 214, the most common adverse reactions (≥20%) reported in patients treated with OPDIVO plus YERVOY (n=547) vs sunitinib (n=535) were fatigue (58% vs 69%), rash (39% vs 25%), diarrhea (38% vs 58%), musculoskeletal pain (37% vs 40%), pruritus (33% vs 11%), nausea (30% vs 43%), cough (28% vs 25%), pyrexia (25% vs 17%), arthralgia (23% vs 16%), and decreased appetite (21% vs 29%). In Checkmate 142 in MSI-H/dMMR mCRC patients receiving OPDIVO as a single agent, the most common adverse reactions (≥20%) were fatigue (54%), diarrhea (43%), abdominal pain (34%), nausea (34%), vomiting (28%), musculoskeletal pain (28%), cough (26%), pyrexia (24%), rash (23%), constipation (20%), and upper respiratory tract infection (20%). In Checkmate 142 in MSI-H/dMMR mCRC patients receiving OPDIVO with YERVOY, the most common adverse reactions (≥20%) were fatigue (49%), diarrhea (45%), pyrexia (36%), musculoskeletal pain (36%), abdominal pain (30%), pruritus (28%), nausea (26%), rash (25%), decreased appetite (20%), and vomiting (20%).

In a separate Phase 3 study of YERVOY 3 mg/kg, the most common adverse reactions (≥5%) in patients who received YERVOY at 3 mg/kg were fatigue (41%), diarrhea (32%), pruritus (31%), rash (29%), and colitis (8%).

Please see U.S. Full Prescribing Information for OPDIVO and YERVOY, including Boxed WARNING regarding immune-mediated adverse reactions for YERVOY.

Applied BioMath, LLC Announces Collaboration with Revitope for Mechanistic PK/PD Modeling in Solid Tumors

On July 10, 2018 Applied BioMath (www.appliedbiomath.com), the industry-leader in applying mechanistic modeling, simulation, and analysis to de-risk and accelerate drug research and development, reported a collaboration with Revitope for an in-vitro and human mechanistic PK/PD modeling of Revitope’s bispecific T Cell Engaging Antibody Circuits (TEAC) targeting solid tumors (Press release, Applied BioMath, JUL 10, 2018, View Source [SID1234633659]). "TEAC are designed to increase tumor specificity and launch an immune activation only when bound to the cancer cell surface. This innovative engineering approach has the potential to unleash potent immune responses that are focused entirely on the tumor," said Werner Meier, CSO and acting CEO of Revitope Oncology. "Our goal in this collaboration is to leverage Applied BioMath’s modeling and analyses capabilities to identify TEAC drug properties that drive the potential for a better therapeutic index and ideally more efficacy in immuno-oncology."

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Applied BioMath employs a rigorous fit-for-purpose model development process, referred to as Model-Aided Drug Invention (MADI), which aims to quantitatively integrate knowledge about therapeutics with an understanding of its mechanism of action in the context of human disease mechanisms. Their MADI approach employs proprietary algorithms and software that were designed specifically for mechanistic PK/PD modeling. "Our mechanistic modeling approach allows our collaborators to assess the feasibility of their therapeutic much more quickly than if they were to rely on experiments alone," said Dr. John Burke, PhD, Co-Founder, President, and CEO of Applied BioMath. "They’ll be able to quickly answer strategic questions about the ideal properties for their therapeutic concept and help accelerate development in Lead Generation and by prioritizing experiments, thus helping them get into the clinical faster and for less money with potentially a BIC therapeutic, giving themselves a much higher chance of clinical success and maximizing R&D ROI."

Adlai Nortye Announce Global License Agreement for Buparlisib (BKM120)

On July 10, 2018 Adlai Nortye Biopharma Co., Ltd. ("Adlai Nortye" or "the Company"), a biopharmaceutical company dedicated to discovering and commercializing new drugs in the field of oncology/immuno-oncology, announced today that it has entered into a Global License Agreement ("the Agreement") with Novartis Pharma AG, a global pharmaceutical company (Press release, Adlai Nortye Biopharma, JUL 10, 2018, View Source [SID1234556283]). Under the terms of the Agreement, except for certain rights maintained by Novartis Pharma AG, Adlai Nortye will have exclusive development and commercialization rights to buparlisib worldwide for all the therapeutic, prophylactic and/or diagnostic uses in humans.

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Buparlisib (BKM120) is an oral pan-PI3K inhibitor that targets all class 1 PI3K isoforms and is active in both hematologic malignancies and solid tumors. It has shown promising efficacy in combination with paclitaxel in head and neck squamous cell carcinoma (HNSCC) and has received a Fast-Track designation from the FDA.

"Combination of buparlisib and paclitaxel demonstrated improved clinical efficacy with a manageable safety profile in patients with HNSCC compared to paclitaxel alone," said Dr. Lars Birgerson, Chief Development Officer of Adlai Nortye and President & CEO of Adlai Nortye USA Inc. "We believe that buparlisib will be another key component in furthering development of our oncology pipeline, and it has great potential for future application in cancer treatment."

"Buparlisib has been extensively profiled in breast cancer and other tumor types. Buparlisib when combined with other therapies has shown impressive anti-cancer efficacy in HNSCC," said Carsten Lu, CEO of Adlai Nortye, "It has very good market prospects when combined with paclitaxel, and we are planning to carry out clinical trials of combination of buparlisib and immune check point inhibitor treatment."

ArQule Announces Commencement of Proposed Public Offering of Common Stock

On July 10, 2018 ArQule, Inc. (Nasdaq: ARQL) reported that it has commenced an underwritten public offering, subject to market and other conditions, to issue and sell shares of its common stock (Press release, ArQule, JUL 10, 2018, View Source [SID1234532697]). In connection with the offering, ArQule expects to grant the underwriters a 30-day option to purchase up to an additional 15% of the shares of its common stock offered in the public offering. There can be no assurances as to whether or when the offering may be completed, or as to the actual size or terms of the offering. All of the shares in the offering are to be sold by ArQule.

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The Company intends to use the net proceeds of the offering to fund its core clinical programs and for general corporate purposes.

Leerink Partners is acting as sole book-running manager for the offering. Needham & Company is acting as lead manager, and Roth Capital Partners, B. Riley FBR, Inc. and JonesTrading Institutional Services LLC are acting as co-managers for the offering.

The securities described above are being offered by ArQule pursuant to a shelf registration statement on Form S-3 (File. No. 333-213456), including a base prospectus, that was previously filed by ArQule with the Securities and Exchange Commission ("SEC") and declared effective on October 5, 2016. The offering is being made only by means of a written prospectus and prospectus supplement that form a part of the registration statement. A preliminary prospectus supplement and accompanying prospectus relating to the offering will be filed with the SEC and will be available on the SEC’s website located at www.sec.gov. Copies of the preliminary prospectus supplement and the accompanying prospectus relating to the offering, when available, also may be obtained from Leerink Partners LLC, Attention: Syndicate Department, One Federal Street, 37th Floor, Boston, MA 02110, by telephone at (800) 808-7525, ext. 6132, or by email at [email protected].

This press release does not constitute an offer to sell or the solicitation of an offer to buy, nor will there be any sales of these securities in any jurisdiction in which such offer, solicitation or sale would be unlawful prior to registration or qualification under the securities laws of such jurisdiction.

VOLUNTARY ANNOUNCEMENT PRODUCT CO-DEVELOPMENT AND STRATEGIC COLLABORATION AGREEMENT

On July 10, 2018 CSPC Pharmaceutical Group Limited (the "Company") is reported that the Company has entered into a product co-development and strategic collaboration agreement (the "Agreement") with Shanghai Junshi Biosciences Co., Ltd. ("Junshi") in relation to the clinical development, registration and commercialization of PD-1 (the anti-PD-1 monoclonal antibody exclusively supplied by Junshi) in combination with albumin-bound paclitaxel for the treatment of breast cancer (the "Product") (Press release, CSPC Pharmaceutical, JUL 10, 2018, View Source [SID1234532266]).

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Pursuant to the Agreement, the Company and Junshi shall form a joint research committee to (1) formulate clinical strategy for the development of the Product; (2) establish and monitor the clinical trials timeline and progress; (3) ensure the full access of clinical data by both parties; (4) discuss and make decision on combination studies of PD-1 with albumin-bound paclitaxel and other chemotherapeutic agents; and (5) resolve any issues that arise during the process of the development and registration of the Product.

The Company shall be responsible for (1) designing and executing clinical trials for the Product; (2) supplying albumin-bound paclitaxel to conduct clinical trials of the Product in the People’s Republic of China (including Hong Kong, Taiwan and Macau) (the "Territory"); (3) applying and securing approval of the Product in the Territory; and (4) commercialization of the Product in the Territory.

Junshi shall be responsible for (1) securing approval of PD-1 single entity in the Territory; (2) supplying PD-1 for the Company to conduct clinical trials for the Product in the Territory; (3) supplying PD-1 to the Company for sales of the Product in the Territory according to a supply agreement to be mutually agreed between the parties.

Junshi grants to the Company a royalty-bearing exclusive license to commercialize the Product in the Territory for a term commencing from the date of the Agreement until 20 years from the receipt of the relevant regulatory approval in the Territory (the "Term"), which allows the Company during the Term to (1) perform clinical and non-clinical studies of the Product; (2) apply for and obtain approvals of the Products in the Territory; and (3) market and sell the Product in the Territory.

Junshi and its affiliates shall not grant any right or license of its PD-1 to any third party for the purpose of development and commercialization of the Product in the Territory. The Company and its affiliates shall only collaborate with Junshi to develop and commercialize the Product.

The Company agrees to pay to Junshi a milestone payment of RMB30,000,000 at each of the five milestone events (i.e. up to an aggregate of RMB150,000,000) leading to the product approval and issuance of product licence by the China Drug Administration for the Product.

All intellectual property rights related to the Product, to the extent solely discovered, invented or developed under the Agreement, shall be jointly owned by the Company and Junshi.