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Olverembatinib

Phase 3

GIST | Small molecule | Oncology |Ascentage Pharma Group International - American Depository Shares|Last Updated: Jul 23, 2026

Target and mechanism

Molecular targetABL1, BCR
Target classInhibitor
ModalitySmall molecule

Also known as Olverembatinib 20mg

Success Probability

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Market & Valuation

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Trial Design

UNCONTROLLED
Total Trials1
Total Enrollment40

FDA Designations

No designations recorded

Clinical trial landscape

Olverembatinib · 4 trials · 8 indications

Phase 3 3Phase 1 1
NCT06640361A Study of Olverembatinib in SDH-deficient GIST.GIST
RECRUITING40 Analytics
NCT06423911Study of Olverembatinib (HQP1351) in Patients With CP-CMLChronic Myeloid Leukemia
RECRUITING285 Analytics
NCT06051409A Study of Olverembatinib in Patients With Newly Diagnosed Ph+ ALL (POLARIS-1)Ph+ ALL
RECRUITING350 Analytics
PHASE3RECRUITING
A Study of Olverembatinib in SDH-deficient GIST.
GISTUnlock trial analytics
PHASE3RECRUITING
Study of Olverembatinib (HQP1351) in Patients With CP-CML
Chronic Myeloid LeukemiaUnlock trial analytics
PHASE3RECRUITING
A Study of Olverembatinib in Patients With Newly Diagnosed Ph+ ALL (POLARIS-1)
Ph+ ALLUnlock trial analytics

Study Endpoints

Primary Endpoints

Progression-free survival(PFS) rate
36 months

Proportion of subjects who do not experience disease progression or death after the first dose of treatment as assessed by Independent Review Committee.

MMR rate Part A
24 weeks

To compare the major molecular response (MMR) rate at 24 weeks of olverembatinib versus bosutinib

MMR rate Part B
24 weeks

To evaluate the MMR rate by 24 weeks of olverembatinib in CML-CP patients with T315I mutation

Minimal Residual Disease Negative CR Rate
Cycle 1 to Cycle 3 (each cycle is 28 days)

The minimal residual disease negative CR rate of olverembatinib combined with chemotherapy versus investigator's choice of TKI combined with chemotherapy in subjects with newly diagnosed Ph+ALL.

Maximum observed plasma concentration C(max)
Day 1 to Day 9

The C(max) of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated and compared.

Time to C(max) [ t(max) ]
Day 1 to Day 9

The t(max) of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated.

Apparent terminal elimination half-life (t½)
Day 1 to Day 9

The t½ of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated.

Area under the concentration-time curve from time zero to last time of quantifiable concentration [AUC(last)]
Day 1 to Day 9

The AUC(last) of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated and compared.

Area under the concentration-time curve from time zero to 192h AUC(0-192h)
Day 1 to Day 9

The AUC(0-192h) of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated and compared.

Apparent Clearance (CL/F)
Day 1 to Day 9

The CL/F of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated.

Apparent Volume of distribution (Vz/F)
Day 1 to Day 9

The Vz/F of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated.

Unbound Fraction (fu)
Day 1 to Day 9

The unbound fraction (fu) of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated.

Secondary Endpoints

Plasma concentrations of olverembatinib
Cycle 2 to Cycle 3 (each cycle is 28 days)
Number of participants with treatment-related adverse events as assessed by CTCAE v5.0.
Through study completion,an average of 2 years.
Event-free Survival (EFS)
Baseline up to 3 to 6 years
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
OlverembatinibEXPERIMENTAL -
Part A, RCT, olverembatinib arm and bosutinib armOTHERRandomized controlled part that is designed to compare the efficacy and safety of olverembatinib (investigational arm) versus bosutinib (control arm) in patients with CML-CP, previously treated with at least two TKIs
Part B, SAT, olverembatinib armOTHERTo evaluate the efficacy and safety of olverembatinib in the CML-CP patients with T315I mutation previously
Investigator's choice of TKIACTIVE_COMPARATORInvestigator's choice of TKI in combination with chemotherapy
Group 1: 6-8 participants with mild hepatic impairment.EXPERIMENTAL -
Group 2: 6-8 participants with normal hepatic function matched to Group 1EXPERIMENTAL -
Group 3: 6-8 participants with moderate hepatic impairmentEXPERIMENTAL -
Group 4: 6-8 participants with normal hepatic function matched to Group 3EXPERIMENTAL -
Group 5: 6-8 participants with severe hepatic impairmentEXPERIMENTAL -
Group 6: 6-8 participants with normal hepatic function matched to Group 5EXPERIMENTAL -

Interventions

NameTypeDescription
OlverembatinibDRUGOral administration with meal, QOD, every 28 days for a cycle.
BosutinibDRUGBosutnib QD
Investigator's choice of TKIDRUGOral (PO) once daily (QD).
Olverembatinib 20mgDRUGorally after meal, single dose
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Eligibility Criteria

Age Range12 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites1

Inclusion Criteria: 1. Histologically and/or cytologically confirmed GIST, immunohistochemistry with loss of SDHB expression, and failure of at least one prior systemic therapy. Defined as disease progression or intolerable as judged by the investigator. 2. Must have at least one measurable target ...

Countries:ChinaUnited StatesAustraliaCzechiaFranceItalyRomaniaSingaporeSouth KoreaSpainTurkey (Türkiye)United Kingdom
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Recent Changes (Last 90 Days)

MEDIUMAug 1, 2026NCT06051409primaryCompletionDate: changed
LOWAug 1, 2026NCT06640361lastUpdatePostDate: changed
MEDIUMAug 1, 2026NCT07282093primaryCompletionDate: changed
MEDIUMAug 1, 2026NCT06423911primaryCompletionDate: changed
MEDIUMAug 1, 2026NCT07282093primaryCompletionDate: changed
MEDIUMAug 1, 2026NCT06423911primaryCompletionDate: changed
MEDIUMAug 1, 2026NCT06051409primaryCompletionDate: changed
LOWAug 1, 2026NCT06640361lastUpdatePostDate: changed
MEDIUMAug 1, 2026NCT07282093primaryCompletionDate: changed
MEDIUMAug 1, 2026NCT06051409primaryCompletionDate: changed
MEDIUMAug 1, 2026NCT06423911primaryCompletionDate: changed
LOWAug 1, 2026NCT06640361lastUpdatePostDate: changed

Frequently asked questions about Olverembatinib

What is Olverembatinib used for?

Olverembatinib is an investigational small molecule being studied for use in oncology. It is in clinical development for Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), chronic myeloid leukemia (CML), gastrointestinal stromal tumors (GIST), and pharmacokinetic studies. It is not yet approved and remains in clinical trials.

What does Olverembatinib target?

Olverembatinib targets ABL1 and BCR, acting as an inhibitor of these molecular targets. This mechanism is relevant to its study in BCR-ABL positive leukemias such as Ph+ ALL and chronic myeloid leukemia. The drug is a small molecule designed to interfere with the activity of these proteins.

Who makes Olverembatinib?

Olverembatinib is being developed by Ascentage Pharma Group International, whose American Depository Shares trade under the ticker AAPG. The company is conducting clinical trials of this investigational drug across multiple oncology indications, including leukemia and gastrointestinal stromal tumors.

What phase is Olverembatinib in?

Olverembatinib is in Phase 3 clinical development for Ph+ ALL, chronic myeloid leukemia, and GIST. It is also being studied in a Phase 1 pharmacokinetic trial. The drug is investigational and has not been approved by regulatory authorities, as it is still undergoing clinical evaluation.

What clinical trials is Olverembatinib in?

Olverembatinib is being studied in several trials. NCT06051409 is a Phase 3 study in newly diagnosed Ph+ ALL. NCT06423911 is a Phase 3 study in chronic-phase CML. NCT06640361 is a Phase 3 study in SDH-deficient GIST. NCT07282093 is a Phase 1 pharmacokinetic study in participants with hepatic impairment.

Is Olverembatinib the same as Olverembatinib 20mg?

Yes, Olverembatinib 20mg refers to the same drug, Olverembatinib. The 20mg designation indicates a specific dosage strength of the medication. This naming is used in some contexts to specify the formulation, but it is the same investigational compound being developed by Ascentage Pharma.