A GBT021601 ADME Microtracer Study in Healthy Volunteers

Data reported in microgram equivalent per milliliter (mcgEq/mL).

Data are reported as aggregate of all scheduled time points.

Data are reported as aggregate of all scheduled time points.

Area under the plasma concentration-time curve up to 24 hours post dose. Data reported in Hour*microgram/millimeter (h*mcg/mL).

Area under the plasma concentration-time curve up to 24 hours postdose. Data reported in hour*microgram equivalent/milliliter (h*mcgEq/mL).

Area under the plasma concentration-time curve from time 0 to infinity calculated as: AUC0-inf=AUC0-t+Clast/kel, where Clast is the last measurable plasma concentration.

Area under the plasma concentration-time curve from time 0 to infinity calculated as: AUC0-inf=AUC0-t+Clast/kel, where Clast is the last measurable plasma concentration and Kel is apparent terminal elimination rate constant.

Apparent terminal elimination half-life, calculated as 0.693/kel where kel is Apparent terminal elimination rate constant.

Apparent terminal elimination half-life, calculated as 0.693/kel where kel is Apparent terminal elimination rate constant.

Renal clearance was calculated as CLR = Ae0-inf/AUC0-inf. Where Ae indicates Cumulative amount of drug excreted and AUC0-inf indicates Area under the plasma concentration-time curve from time 0 to infinity.

Apparent volume of distribution at terminal phase, calculated as: (CL/F) Apparent total clearance, calculated as dose/AUC0-inf/Kel.

Apparent volume of distribution at terminal phase, calculated as: (CL/F) Apparent total clearance, calculated as dose/AUC0-inf/Kel.

Apparent total clearance, calculated as dose/AUC0-inf.

Apparent total clearance, calculated as dose/AUC0-inf.

An Adverse event (AE) was any unfavourable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medical treatment or procedure that may or may not be considered related to the medical treatment or procedure. TEAEs were those which occurred (or worsened) after the dose of study drug during the on-treatment period, defined as the period after the dose of study drug and through the minimum of (Study Day 57, study discontinuation).

Blood and urine samples was collected for clinical laboratory assessments. Clinical Laboratory Values included Clinical chemistry: alanine aminotransferase, albumin, alkaline phosphatase, aspartate aminotransferase, bicarbonate, bilirubin (total, direct, and indirect), blood urea nitrogen, calcium, chloride, creatinine, gamma glutamyl transferase, glucose, lactate dehydrogenase, magnesium, phosphorus, potassium, sodium, total protein, and uric acid. Hematology: leukocytes, erythrocytes, hematocrit, Hb, mean corpuscular volume, mean corpuscular hemoglobin, mean corpuscular hemoglobin concentration, platelet count (ie, thrombocytes), RBC count, and white blood cell count etc. Urinalysis: determination of pH and specific gravity, and presence of bilirubin, blood, glucose, ketones, nitrite, protein, leukocytes, and urobilinogen etc. Coagulation, Serology, Drug and alcohol screen and Pregnancy test. Clinical significance was judged by investigator.

Systolic and diastolic blood pressure and pulse was recorded after the participant had rested for at least 5 minutes in the supine position. Body temperature and respiratory rate was also measured. Clinical significance was judged by investigator.

Standard 12-lead ECGs were performed after the participant had rested quietly for more than 5 minutes in a supine position utilizing an ECG machine that was equipped with computer-based interval measurements. The following measurement was recorded: the heart rate (of <45 or >100 beats per minute (BPM) , PR interval, QT interval, QT interval corrected using Fridericia's formula (QTcF) of >450 msec for males and >470 msec for females, and QRS duration. Any cardiac rhythm other than sinus rhythm that was interpreted by the Investigator was clinically significant.

Physical Examination test included body weight and height. physical examination was conducted at screening. Clinical significance was judged by investigator.