Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Also known as [14]-AST2818, AST2818 Tablets, Firmonertinib, Furmonertinib
AST2818 · 12 trials · 20 indications
Safe import period
Safe import period
Randomized Controlled Phase：PFS assessed by BICR based on recist1.1; PFS was defined as the time from the date of randomization to the date of first documented disease progression (assessed according to RECIST v1.1 criteria) or death from any cause, whichever occurred first.
Disease free survival
PFS is defined as the time from randomization to the first occurrence of disease progression as determined by BICR using RECIST v1.1, or death from any cause, whichever occurs first.
Confirmed ORR is defined as the percentage of participants with a confirmed CR or PR based on BICR assessment relative to the total number of participants.
DFS as assessed by the investigator in Stage II- IIIB. DFS defined as the time from the date of randomization to the first observation of disease recurrence (by pathological diagnosis or imaging) or death caused by any reason, whichever occurs first.
The time from the date of randomization to the date of first documentation of disease progression (assessed according to RECIST v1.1 criteria) or death from any cause, whichever occurred first.
Percentage of patients with a confirmed CR or PR relative to the total number of patients.
Pharmacokinetics of AST2818 by assessment of maximum plasma AST2818 concentration.
Pharmacokinetics of AST2818 by assessment of area under the plasma concentration time curve from zero to appointed time
Pharmacokinetics of AST2818 by assessment of time to Cmax.
The percentage of radioactive dose of \[14C\] radiolabelled AST2818 recovered in blood and in total, up to Day 85（p.s:The administration time on the first day is 7:30 am）
The percentage of radioactive dose of \[14C\] radiolabelled AST2818 recovered in urine, faeces and in total, up to Day 85（p.s:The administration time on the first day is 7:30 am）
The concentrations of AST2818 and AST5902 in plasma up to Day 85（p.s:The administration time on the first day is 7:30 am）
Proportion of different metabolites
Types of adverse events
| Arm | Type | Description |
|---|---|---|
| Furmonertinib combined with chemotherapy | EXPERIMENTAL | Furmonertinib Mesilate Tablets+Carboplatin Injection/Cisplatin for injection+Pemetrexed Disodium for Injection |
| Osimertinib Mesylate Tablets | ACTIVE_COMPARATOR | Osimertinib Mesylate Tablets |
| Furmonertinib | EXPERIMENTAL | Furmonertinib (80 mg orally, once daily), in accordance with the randomization schedule. |
| Placebo Furmonertinib | PLACEBO_COMPARATOR | Matching placebo for Furmonertinib (80 mg orally, once daily), in accordance with the randomization schedule. |
| Firmonertinib 240 mg | EXPERIMENTAL | - |
| EGFR-TKI inhibitor osimertinib or afatinib based on investigator's choice | ACTIVE_COMPARATOR | - |
| Firmonertinib | EXPERIMENTAL | Firmonertinib: 240 mg, QD, orally |
| Placebo | PLACEBO_COMPARATOR | Placebo: 240 mg, QD, orally |
| chemotherapy | ACTIVE_COMPARATOR | Pemetrexed Disodium for Injection： 500mg/m2, intravenous infusion. Cisplatin for injection：75 mg/m2， intravenous infusion. Carboplatin Injection：administered according to the AUC of 5 mg/ml, intravenous infusion. |
| furmonertinib 240 mg | EXPERIMENTAL | - |
| furmonertinib 160 mg | EXPERIMENTAL | - |
| platinum-based chemotherapy | ACTIVE_COMPARATOR | carboplatin or cisplatin based on investigator's choice + pemetrexed intravenously |
| Furmonertinib 240mg QD | EXPERIMENTAL | Treating patients of locally advanced or metastatic NSCLC with EGFR exon 20 insertions who have progressed during or after platinum-based chemotherapy. |
| Group A: Furmonertinib 80mg QD | EXPERIMENTAL | Furmonertinib (AST2818) 80mg QD. All patients enrolled into this group will receive furmonertinib 80mg daily. |
| Group B1: Furmonertinib 80mg QD | EXPERIMENTAL | Furmonertinib (AST2818) 80mg QD. All patients enrolled into this group will receive furmonertinib 80mg daily. |
| Group B2: Furmonertinib plus chemotherapy | EXPERIMENTAL | Furmonertinib 80 mg QD and platinum-based chemotherapy All patients enrolled into this group will receive furmonertinib 80 mg daily, in combination with Pemetrexed (500 mg/m2) plus carboplatin (AUC 5) on Day 1 of 21day cycles (every 3 weeks) for 4 cycles, followed by pemetrexed maintenance (500 mg/m2) every 3 weeks. |
| Group B3: Furmonertinib plus chemotherapy and bevacizumab | EXPERIMENTAL | Furmonertinib 80 mg QD plus platinum-based chemotherapy and bevacizumab All patients enrolled into this group will receive furmonertinib 80 mg daily, in combination with Pemetrexed (500 mg/m2) plus carboplatin (AUC 5) plus bevacizumab (7.5mg/kg) on Day 1 of 21day cycles (every 3 weeks) for 4 cycles, followed by pemetrexed (500 mg/m2) with bevacizumab (7.5mg/kg) maintenance every 3 weeks. |
| Fasted AST2818 tablets following a period of fasting | EXPERIMENTAL | - |
| High-fat meal AST2818 tablets following a high-fat meal | EXPERIMENTAL | - |
| treated subjects will receive Furmonertinib 160mg/day, | EXPERIMENTAL | treated subjects will receive Furmonertinib 160mg/day, QD, PO, under fasted state, until progressive disease, death or intolerability. |
| treated subjects will receive Furmonertinib 240mg/day, | EXPERIMENTAL | treated subjects will receive Furmonertinib 160mg/day, QD, PO, under fasted state, until progressive disease, death or intolerability. |
| treatment-naïve subjects will receive Furmonertinib 240mg/day | EXPERIMENTAL | Treatment naïve patients with EGFR exon 20 insertion mutation positive NSCLC |
| [14C]-AST2818 80mg (oral solution) | EXPERIMENTAL | Volunteers will receive 80 mg \[14C\]-AST2818 containing a nominal 100 μCi activity, administered by mouth, as a solution. |
| Stage 1 Dose Escalation and Backfill | EXPERIMENTAL | Experimental: Previously treated patients with advanced or metastatic NSCLC with activating EGFR or HER2 mutations |
| Stage 2 Expansion Cohort 1 | EXPERIMENTAL | Previously Treated NSCLC Patients with EGFR Exon 20 Insertion Mutations |
| Stage 2 Expansion Cohort 2 | EXPERIMENTAL | Previously treated NSCLC Patients with HER2 Exon 20 Insertion Mutations |
| Stage 2 Expansion Cohort 3 | EXPERIMENTAL | Previously treated NSCLC Patients with EGFR Activating Mutations, who are not eligible for Cohorts 1 and 4 |
| Stage 2 Expansion Cohort 4 | EXPERIMENTAL | Untreated or Previously treated EGFR TKI Naïve NSCLC Patients with EGFR Uncommon Mutations, excluding EGFR exon 20 insertion mutations |
| Name | Type | Description |
|---|---|---|
| Furmonertinib Mesilate Tablets | DRUG | Usage and dosage: 80mg, 240mg, or 160mg QD orally Medication duration: A cycle of 21 days until intolerable toxicity, disease progression, death, or initiation of new anti-tumor therapy occurs |
| Carboplatin Injection | DRUG | Usage and dosage: Administer via IV infusion, with a dosage of AUC5, not exceeding 750 mg. Medication schedule: every 3 weeks as a cycle, D1 administration per cycle, immediate administration of carboplatin upon completion of pemetrexed infusion, intravenous infusion, carboplatin can be used for up to 4 cycles. |
| Cisplatin for injection | DRUG | Usage and dosage: Administer via IV infusion at a dose of 75 mg/m2. Medication schedule: Every 3 weeks as a cycle, with D1 administration per cycle. Cisplatin is administered approximately 30 minutes after the infusion of pemetrexed, via intravenous infusion. Adequate hydration therapy must be received before and after cisplatin treatment. Cisplatin can be used for up to 4 cycles. |
| Pemetrexed Disodium for Injection | DRUG | Usage and dosage: Intravenous (IV) infusion administration, dosage of 500 mg/m2 Medication schedule: Administer on the first day of each cycle (21 days per cycle, i.e. every 3 weeks) until intolerable toxicity, disease progression, death, or initiation of new anti-tumor therapy occurs. |
| Osimertinib Mesylate Tablets | DRUG | Usage and dosage: 80mg, QD administration Medication duration: A cycle of 21 days until intolerable toxicity, disease progression, death, or initiation of new anti-tumor therapy occurs |
| Drug: Furmonertinib 80 mg | DRUG | The initial dose of Furmonertinib 80 mg once daily |
| Furmonertinib 80 mg placebo | DRUG | The initial dose of Furmonertinib 80 mg once daily |
| Firmonertinib | DRUG | 240 mg oral, daily firmonertinib tablet |
| EGFR-TKI inhibitor based on investigator's choice | DRUG | osimertinib 80 mg oral, daily tablet OR afatinib 40 mg oral, daily tablet |
| Placebo | DRUG | Placebo: 240 mg, QD, orally |
| Firmonertinib Mesilate Tablets | DRUG | Usage and dosage: oral, 240mg, QD。 Medication duration: 21 days as a cycle, until intolerable toxicity, loss of clinical benefit, disease progression (confirmed by BICR), death or other anti-tumor treatment (whichever occurs first). |
| furmonertinib 240 mg oral, daily | DRUG | furmonertinib tablet |
| furmonertinib 160 mg oral, daily | DRUG | furmonertinib tablet |
| platinum-based chemotherapy | DRUG | (carboplatin or cisplatin based on investigator's choice) + pemetrexed intravenously (IV) |
| Furmonertinib | DRUG | 240mg QD on a continuous dosing schedule. |
| Furmonertinib/Pemetrexed/Carboplatin | DRUG | Furmonertinib 80mg daily + Pemetrexed (500 mg/m2) plus carboplatin (AUC 5) on Day 1 of 21day cycles (every 3 weeks) for 4 cycles, followed by pemetrexed maintenance (500 mg/m2) every 3 weeks. |
| Furmonertinib/Pemetrexed/Carboplatin/Bevacizumab | DRUG | Furmonertinib 80mg daily + Pemetrexed (500 mg/m2) plus carboplatin (AUC 5) plus bevacizumab (7.5mg/kg) on Day 1 of 21day cycles (every 3 weeks) for 4 cycles, followed by pemetrexed (500 mg/m2) with bevacizumab (7.5mg/kg) maintenance every 3 weeks. |
| AST2818 Tablets | DRUG | AST2818 Tablets: Period 1 Fasted from 10 hours prior to dosing with 80 mg AST2818 tablet (p o, once) and 4 hours after dosing on day 1. Period 2 Allocated high-fat meal prior to dosing with 80 mg AST2818 tablet (p o, once) and fasted 4 hours after dosing on day 1. |
| Furmonertinib 160mg | DRUG | randomized to 160mg QD |
| Furmonertinib 240mg | DRUG | randomized to 240mg QD |
| [14]-AST2818 | DRUG | Volunteer will receive a single oral dose of 80 mg /100 u Ci \[14C\]-AST2818 as a solution on Day 1 |
Inclusion Criteria: 1. Fully understand the trial and voluntarily sign the informed consent form; 2. Age ≥18 years at the time of signing ICF, regardless of gender; 3. Histologically/cytologically confirmed non-squamous NSCLC with brain parenchymal metastases assessed by BICR; Subjects with both br...
AST2818 is an investigational small molecule drug developed by ArriVent BioPharma, Inc. (ticker AVBP). It is in Phase 1 clinical development. The specific disease indications for AST2818 have not been disclosed. Two Phase 1 trials of AST2818 have been completed, both in healthy male volunteers in China.
AST2818 is being developed by ArriVent BioPharma, Inc., which trades under the ticker AVBP. The company is responsible for the clinical development of AST2818, which is currently in Phase 1 testing. No partnership or collaboration information for AST2818 has been disclosed.
AST2818 is in Phase 1 clinical development. Two Phase 1 trials have been completed, and no active trials are currently listed. The completed trials enrolled a total of 22 healthy male volunteers in China. AST2818 has not been approved by the FDA or any regulatory agency.
AST2818 has been evaluated in two completed Phase 1 trials. NCT03941340 studied the mass balance and biotransformation of a single dose of [14C] AST2818 in six Chinese healthy male volunteers. NCT03926182 assessed the effect of food on blood levels of AST2818 after single oral doses in 16 healthy male volunteers in China.
Yes, AST2818 is also known as [14]-AST2818 and AST2818 Tablets. These alternative names refer to the same investigational drug developed by ArriVent BioPharma, Inc. The [14C] label denotes a radiolabeled version used in a mass balance study, while AST2818 Tablets refers to the oral tablet formulation.