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DRUG:

BLU-701

i
Other names: BLU-701, ZL-2314
Company:
Blueprint Medicines, ZAI Lab
Drug class:
EGFR inhibitor
Related drugs:
over1year
(HARMONY) Study of BLU-701 in EGFR-mutant NSCLC (clinicaltrials.gov)
P1/2, N=20, Terminated, Blueprint Medicines Corporation | N=160 --> 20 | Trial completion date: Dec 2024 --> Dec 2022 | Active, not recruiting --> Terminated | Trial primary completion date: Jun 2024 --> Dec 2022; Lack of efficacy
Enrollment change • Trial completion date • Trial termination • Trial primary completion date
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion
|
Tagrisso (osimertinib) • carboplatin • pemetrexed • BLU-701
almost2years
(HARMONY) Study of BLU-701 in EGFR-mutant NSCLC (clinicaltrials.gov)
P1/2, N=160, Active, not recruiting, Blueprint Medicines Corporation | Recruiting --> Active, not recruiting
Enrollment closed
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion
|
Tagrisso (osimertinib) • carboplatin • pemetrexed • BLU-701
2years
BLU-945 or BLU-701 as single agents versus their combination with osimertinib in EGFR L858R driven tumor models (AACR-NCI-EORTC 2022)
The in vivo antitumor activities of BLU-945 and BLU-701 as single agents suggest both BLU-945 and BLU-701 have the potential to be used as 1L therapy in patients with EGFR L858R-driven NSCLC. The superior in vivo antitumor activity of BLU-945 or BLU-701 in combination with osimertinib in prolonging the DOR or increasing tumor growth inhibition in these models may have clinical application in improving outcomes of patients with EGFR L858R-driven NSCLC in 1L settings.
Preclinical
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR wild-type • EGFR C797S
|
Tagrisso (osimertinib) • tigozertinib (BLU-945) • BLU-701
almost3years
BLU-701 tumour suppression and intracranial activity as a single agent and in combination with BLU-945 in models of non-small cell lung cancer (NSCLC) driven by EGFR mutations (BTOG 2022)
Consistent with its brain penetration properties, BLU-701 exhibited dose-dependent brain tumour inhibition that surpassed gefitinib and erlotinib in an EGFR ex19del PC9-luc CDX model in which cells were implanted intracranially or inoculated in the carotid artery (followed by migration to the brain). The in vivo activity of BLU-701 supports its potential as a treatment for patients with EGFR-mutated NSCLC, including those with the C797S mutation resistant to covalent 3rd-generation TKIs, such as osimertinib. Its intracranial penetrance and brain tumour response suggest potential benefits in treating and/or preventing brain metastases. Broader EGFR mutational coverage could be achieved with BLU-701 and BLU-945 in combination, which could potentially prolong responses.
Combination therapy
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR exon 19 deletion • EGFR T790M • EGFR wild-type • EGFR C797S
|
Tagrisso (osimertinib) • erlotinib • gefitinib • tigozertinib (BLU-945) • BLU-701
almost3years
(HARMONY) Study of BLU-701 in EGFR-mutant NSCLC (clinicaltrials.gov)
P1/2, N=160, Recruiting, Blueprint Medicines Corporation | Not yet recruiting --> Recruiting
Enrollment open
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion
|
Tagrisso (osimertinib) • carboplatin • pemetrexed • BLU-701
almost3years
(HARMONY) Study of BLU-701 in EGFR-mutant NSCLC (clinicaltrials.gov)
P1/2, N=160, Not yet recruiting, Blueprint Medicines Corporation
New P1/2 trial
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion
|
Tagrisso (osimertinib) • carboplatin • pemetrexed • BLU-701