We own or control all commercial rights in our darovasertib program in UM, including in MUM and in primary UM, subject
to certain economic obligations pursuant to our exclusive, worldwide license with Novartis to darovasertib.
IDE397MAT2A Inhibitor in Tumors with MTAP
Deletion
IDE397, our small molecule methionine adenosyltransferase 2a, or MAT2A, inhibitor, is being evaluated in a Phase 1/2 clinical trial. We are
actively enrolling into the Phase 2 monotherapy expansion cohort in selected priority indications for patients with tumors with methylthioadenosine phosphorylase, or MTAP, gene deletion, including
squamous non-small cell lung, bladder, gastric and esophageal cancers.
We are collaborating with Amgen Inc., or
Amgen, to clinically evaluate IDE397 in combination with AMG 193, Amgens investigational MTA-cooperative PRMT5 inhibitor, in patients with tumors with MTAP-deletion, in an Amgen-sponsored clinical trial
pursuant to our Clinical Trial Collaboration and Supply Agreement with Amgen. In August 2023, Amgen initiated and dosed the first patient in the IDE397 and AMG 193 combination trial, following FDA authorization to proceed with the clinical trial.
The ongoing Phase 1/2 clinical trial is evaluating the safety, tolerability, pharmacokinetics, pharmacodynamics and efficacy of IDE397 in combination with AMG 193, with an initial focus on expansion in
non-small cell lung cancer, or NSCLC, patients and an anticipated enrollment of approximately 180 patients. Enrollment is ongoing in the dose escalation portion of this Phase 1/2 clinical trial. We intend to
develop a joint publication strategy for the Phase 1/2 clinical trial later in 2024.
We are separately collaborating with Gilead Sciences, Inc., or Gilead, to
clinically evaluate IDE397 in combination with sacituzumab-govitecan-hziy, or Trodelvy, Gileads Trop-2 directed anti-body conjugate, in patients with MTAP deletion
bladder cancer. The IDE397 and Trodelvy combination is being evaluated in an IDEAYA-sponsored Phase 1 clinical trial, which initiated enrollment in June 2024.
Company-Sponsored Phase 2 Monotherapy Expansion in MTAP-Deletion Urothelial and Lung Cancer
In July 2024, we announced clinical data for the IDE397 Phase 2 monotherapy expansion dose demonstrating preliminary clinical efficacy in heavily pre-treated MTAP-deletion urothelial cancer and NSCLC patients. The patients evaluated had a median of two prior lines of therapy, ranging from one to nine prior lines of treatment. The reported Phase 2 clinical
data were based on 18 evaluable MTAP-deletion patients, including seven urothelial cancer patients, four adenocarcinoma NSCLC patients, and seven squamous NSCLC patients at the expansion dose of 30 mg once-a-day, or QD, of IDE397. In the interim update for 18 evaluable patients, with a data analysis cutoff date of June 21, 2024, we reported an overall response rate of approximately 39% (one complete
response and six partial responses by RECIST 1.1 evaluation), which includes two unconfirmed partial responses (one urothelial cancer patient that had a 100% tumor reduction in the target lesion at the last
CT-scan assessment and one adenocarcinoma NSCLC patient). We also observed a disease control rate of 94%, including one complete response, six partial responses and ten stable disease by RECIST 1.1 evaluation.
In addition, we observed tumor shrinkage in 14 of the 18 evaluable patients. 11 of the evaluable patients are still on treatment and five of the seven responses by RECIST 1.1 evaluation remain in response. We also reported a ctDNA molecular
response, or MR, rate of 81%, representing 13 of 16 reportable patients with 50% or greater ctDNA reduction (several quality control failures of patient samples precluded the other patients from MR analysis).
Regarding safety data, we also reported a favorable AE profile at the 30 mg QD expansion dose. Approximately 5.6% of patients experienced a Grade 3 or higher
drug-related AE at the 30 mg QD dose, represented by one instance of Grade 3 asthenia, and no drug-related SAEs were observed. We observed no drug-related AEs