1. To observe the safety and tolerability of oral XY0206 in patients with advanced/metastatic malignant solid tumor in China, and observe the drug dose limiting toxicity (DLT) to establish the maximum tolerated dose (MTD) in humans. 2. To investigate the pharmacokinetic (PK) characteristics, pharmacodynamics (PD) characteristics, and PK/PD correlation of single and multiple doses of XY0206 in patients with advanced/metastatic malignant solid tumors to provide dose selection basis for clinical studies; 3. To evaluate the effect of standard meal on main PK parameters of XY0206; 4. To determine the metabolites of XY0206 in patients with advanced/metastatic malignant solid tumor. 5. To explore the correlation between PK and QTcF. 6. Preliminary investigates the effectiveness of XY0206 in patients with advanced/metastatic malignant solid tumors.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
34
Dosage form:Tablet;Single dose treatment:Take the drug once on day 1,each time 1 tablet. Multiple dose phase:Take the medicine once a day,1 tablet at a time.4 weeks of continuous medication is one course of treatment. After the first course of treatment, the subjects can continue to receive the experimental drug treatment until they meet the criteria for stopping treatment or determine the duration and interval of treatment according to the accumulated condition after multiple dose.
National Cancer Center/Cancer Hospital,Chinese Academy of Medical Sciences and Peking Union Medical College
Beijing, Beijing Municipality, China
RECRUITINGThe First Affiliated Hospital of Hainan Medical College
Haikou, Hainan, China
NOT_YET_RECRUITINGThe Fourth Hospital of Hebei Medical University
Shijiazhuang, Hebei, China
NOT_YET_RECRUITINGTianjin Cancer Hospital
Tianjin, Tianjin Municipality, China
NOT_YET_RECRUITINGDLT
The occurrence of DLT.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
AE
The occurrence rate of AE.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
ADR
The occurrence rate of adverse drug reactions(ADR).
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
SAE
The occurrence rate of SAE.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Blood routine
One of the laboratory tests.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Urine routine
One of the laboratory tests.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Stool routine
One of the laboratory tests.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Blood biochemistry
One of the laboratory tests.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Coagulation function
One of the laboratory tests.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
12 lead ecg
One of the laboratory tests.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Body temperature
One of the vital signs.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Blood pressure
One of the vital signs.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Heart rate
One of the vital signs.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Breathing
One of the vital signs.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
General condition
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Skin
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Head
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Eyes
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Ears
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Nose
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Throat
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Heart
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Lung
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Chest
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Abdomen
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Limbs
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Nerves
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Back/spine
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
Lymph nodes
One of the physical examination.
Time frame: from the start of the medication to the end of the study or 28 days after cessation of medication
AUCinf
area under the concentration-time curve from the time of dosing extrapolated to time infinity.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
AUC0-24h
area under the concentration-time curve from the time of dosing extrapolated to the 24h after dosing.
Time frame: single dose phase:up to 24 hours;multiple dose phase:up to 24 hours
AUC0-72h
area under the concentration-time curve from the time of dosing extrapolated to the 72h after dosing.
Time frame: single dose phase:up to 72 hours
AUC0-120h
area under the concentration-time curve from the time of dosing extrapolated to the 120h after dosing.
Time frame: single dose phase:up to 120 hours
Peak Plasma Concentration (Cmax)
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
CL/F
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
Tmax
The amount of time that a drug is present at the maximum concentration in serum.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
Cmin,ss
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
Cmax,ss
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The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
Cav,ss
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
PTF
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
RAUC1
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
RAUC2
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
RCmax
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
Kel
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
t1/2
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
Vz/F
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
AUC_%Extrap
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 120 hours;multiple dose phase:up to 24 hours
Ae0-24h
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 24 hours;multiple dose phase:up to 24 hours
Fe0-24h
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 24 hours;multiple dose phase:up to 24 hours
Ae0-72h
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 72 hours
Fe0-72h
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 72 hours
Ae0-72h stool
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 72 hours
CLr
The PK parameters of the plasma sample.
Time frame: single dose phase:up to 24 hours;multiple dose phase:up to 24 hours
Exploring the relative baseline change percentage of biomarkers (soluble VEGFR2).
The PD parameters of XY0206.
Time frame: single dose phase:up to 24 hours;multiple dose phase:up to 24 hours
Complete response rate (CRR)
Effective parameters of XY0206.
Time frame: through study completion,such as 30 months.
Partial response rate (PRR)
Effective parameters of XY0206.
Time frame: through study completion,such as 30 months.
Objective response rate (ORR)
Effective parameters of XY0206.
Time frame: through study completion,such as 30 months.
Progression-free survival (PFS)
Effective parameters of XY0206.
Time frame: through study completion,such as 30 months.