Phase 1 N=9 Other

A GBT021601 ADME Microtracer Study in Healthy Volunteers

Sickle Cell Disease

Bottom Line

View on ClinicalTrials.gov: NCT05718687 ↗

Enrolled (actual)

Serious AEs

0.0%

Results posted

Jan 2025

Primary outcome: Primary: GBT021601 Concentration in Whole Blood and Plasma at Predose — NA; NA Microgram/ milliliter (mcg/mL)

Study Design & Population

Study type: Interventional
Phase: Phase 1
Interventions: GBT021601 (Drug)
Age: Adult · 18+ yrs
Sex: All
Sponsor: Pfizer
Primary completion: Aug 2023

Outcome Measures

Outcome	Result	p-value
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at Predose	NA; NA	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at Predose	0; 0	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 0.25 Hours	6.368; 0.46267	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentrations in Whole Blood and Plasma at 0.25 Hours	5.8206; 0.84819	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 0.50 Hours	17.33; 1.2338	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 0.50 Hours	16.45; 2.345	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 1 Hours	29.37; 1.433	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 1 Hours	27.24; 2.913	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 2 Hours	31.92; 0.9228	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 2 Hours	29.52; 2.089	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 3 Hours	31.92; 0.5974	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 3 Hours	29.78; 1.502	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 4 Hours	34.96; 0.4539	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 4 Hours	31.23; 1.2243	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 6 Hours	34.84; 0.3013	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 6 Hours	31.51; 0.8534	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 8 Hours	36.00; 0.2267	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 8 Hours	31.53; 0.6592	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 12 Hours	36.49; 0.1986	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 12 Hours	32.95; 0.5064	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 24 Hours	37.53; 0.1479	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 24 Hours	33.62; 0.3256	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 48 Hours	37.39; 0.1402	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 48 Hours	33.29; 0.2207	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 72 Hours	35.41; 0.1377	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 72 Hours	31.38; 0.1861	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 96 Hours	34.67; 0.12923	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 96 Hours	30.62; 0.1670	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 144 Hours	32.48; 0.11038	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 144 Hours	28.81; 0.1434	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 168 Hours	32.91; 0.12189	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 168 Hours	27.33; 0.1471	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 312 Hours	26.59; 0.11109	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 312 Hours	23.44; 0.1274	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 480 Hours	22.38; 0.08271	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 480 Hours	19.30; 0.09706	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 648 Hours	18.71; 0.07343	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 648 Hours	16.32; 0.08224	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 816 Hours	15.20; 0.06894	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 816 Hours	12.93; 0.08084	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 984 Hours	12.60; 0.05919	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 984 Hours	11.087; 0.06646	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 1320 Hours	8.772; 0.03829	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 1320 Hours	7.599; 0.04387	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 1656 Hours	6.253; 0.02809	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 1656 Hours	5.528; 0.02835	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 1992 Hours	4.283; 0.01881	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 1992 Hours	3.667; 0.01909	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 2328 Hours	2.997; 0.01407	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 2328 Hours	2.677; 0.013250	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 2664 Hours	2.290; NA	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 2664 Hours	2.064; 0.008206	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 3240 Hours	1.1523; NA	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 3240 Hours	0.9463; NA	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 3576 Hours	0.6097; NA	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 3576 Hours	0.6733; NA	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 4248 Hours	NA; NA	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 4248 Hours	0.2745; NA	—
PRIMARY GBT021601 Concentration in Whole Blood and Plasma at 4920 Hours	NA; NA	—
PRIMARY 14C-GBT021601 Total Radioactivity Concentration in Whole Blood and Plasma at 4920 Hours	0.2330; NA	—
PRIMARY Cumulative Amount of [14C]-GBT021601 Total Radioactivity Excreted in Urine and Feces	95.23; 81.38	—
PRIMARY Cumulative Fraction of [14C]-GBT021601 Total Radioactivity Excreted in Urine and Feces	47.24; 40.37	—
PRIMARY Area Under the Plasma Concentration-Time Curve From Time Zero (0) to 24 Hours (AUC0-24) of GBT021601 in Whole Blood and Plasma	824.1; 7.393	—
PRIMARY Area Under the Plasma Concentration-Time Curve From Time Zero (0) to 24 Hours (AUC0-24) of 14C-GBT021601 in Whole Blood and Plasma	741.8; 17.92	—
PRIMARY Area Under the Concentration-Time From Time Zero to the Last Measurable Concentration (AUC0-last) of GBT021601 in Whole Blood and Plasma	31481.7; 130.35	—
PRIMARY Area Under the Concentration-Time From Time Zero to the Last Measurable Concentration (AUC0-last) of 14C-GBT021601 in Whole Blood and Plasma	27609.6; 165.7	—
PRIMARY Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUC0-inf) of GBT021601 in Whole Blood and Plasma	35290.5; 150.7	—
PRIMARY Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUC0-inf) of 14C-GBT021601 in Whole Blood and Plasma	30636.1; 179.1	—
PRIMARY Maximum Observed Concentration (Cmax) of GBT021601 in Whole Blood and Plasma	40.06; 1.468	—
PRIMARY Maximum Observed Concentration (Cmax) of 14C-GBT021601 in Whole Blood and Plasma	34.05; 2.950	—
PRIMARY Time to Attain Maximum Observed Concentration (Tmax) of GBT021601 in Whole Blood and Plasma	24.000; 1.000	—
PRIMARY Time to Attain Maximum Observed Concentration (Tmax) of 14C-GBT021601 in Whole Blood and Plasma	24.000; 1.000	—
PRIMARY Apparent Terminal Elimination Half-Life (t1/2) of GBT021601 in Whole Blood and Plasma	647.8; 707.1	—
PRIMARY Apparent Terminal Elimination Half-Life (t1/2) of 14C-GBT021601 in Whole Blood and Plasma	654.7; 588.9	—
PRIMARY Renal Clearance (CLR) of GBT021601 and 14C-GBT021601 in Urine	0.2755	—
PRIMARY Apparent Volume of Distribution at Terminal Phase (Vz/F) of GBT021601 in Whole Blood and Plasma	5.175; 1300.6	—
PRIMARY Apparent Volume of Distribution at Terminal Phase (Vz/F) of 14C-GBT021601 in Whole Blood and Plasma	5.972; 906.1	—
PRIMARY Apparent Total Clearance (CL/F) of GBT021601 in Whole Blood and Plasma	0.005713; 1.338	—
PRIMARY Apparent Total Clearance (CL/F) of 14C-GBT021601 in Whole Blood and Plasma	0.006580; 1.1258	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 0-6 Hours	13.123	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 6-12 Hours	16.611	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 12-24 Hours	19.70	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 0-24 Hours	0.060486	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 24 Hours	23.19; 24.25	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 48 Hours	25.50; 33.17	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 72 Hours	27.55; 35.06	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 96 Hours	29.35; 37.31	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 120 Hours	30.97; 40.54	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 144 Hours	32.88; 39.51	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 168 Hours	34.82; 40.87	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 192 Hours	36.72; 44.39	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 216 Hours	38.48; 43.09	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 240 Hours	40.22; 43.54	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 264 Hours	41.99; 45.31	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 288 Hours	43.65; 44.72	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 312 Hours	45.06; 46.29	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 336 Hours	46.50; 50.24	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 360 Hours	47.92; 48.56	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 384 Hours	49.41; 52.20	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 408 Hours	50.87; 49.97	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 432 Hours	52.24; 50.84	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 456 Hours	53.59; 53.99	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 480 Hours	54.81; 52.89	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 504 Hours	56.00; 53.22	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 528 Hours	57.15; 56.23	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 552 Hours	58.19; 55.14	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 576 Hours	59.25; 55.39	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 600 Hours	60.20; 58.26	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 624 Hours	61.13; 57.17	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 648 Hours	62.18; 59.51	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 816 Hours	67.24; 62.99	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 984 Hours	74.37; 67.30	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 1320 Hours	83.07; 72.95	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 1656 Hours	89.48; 76.42	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 1992 Hours	93.46; 79.01	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 2328 Hours	92.85; 84.14	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 2664 Hours	100.08; 59.86	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 3240 Hours	98.36; 69.27	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 3576 Hours	98.96; 69.62	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 4248 Hours	93.30; 85.10	—
PRIMARY Distribution of 14C- GBT021601 Total Radioactivity in Urine and Feces at 4920 Hours	96.31; 63.87	—
SECONDARY Number of Participants With Treatment Emergent Adverse Events (TEAEs)	4	—
SECONDARY Number of Participants With Clinically Significant Laboratory Values	—	—
SECONDARY Number of Participants With Clinically Significant Vital Signs Values	—	—
SECONDARY Number of Participants With Clinically Significant ECG Values	—	—
SECONDARY Number of Participants With Clinically Significant Physical Examination Values	—	—

Summary

An Open-label Study of GBT021601 in 8 to 10 healthy male or female participants to evaluate the absorption, distribution, metabolism, and excretion (ADME) of GBT021601.

Eligibility Criteria

Inclusion Criteria

Body mass index (BMI): 18.0 to 27.0 kg/m2, inclusive, at screening.
Body weight ≥ 50 kg at screening
Females must be nonlactating and nonpregnant (as confirmed by a negative serum pregnancy test at screening and admission for all females), or of nonchildbearing potential (ie, either surgically sterilized or physiologically incapable of becoming pregnant, or at least 1 year postmenopausal [defined as at least 12 months no menses, and confirmed by a follicle-stimulating hormone test, at screening]).
Creatinine clearance (glomerular filtration rate) as estimated by the Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) formula: ≥90 mL/min, at screening.

Exclusion Criteria

History or presence of conditions which, in the opinion of the Investigator, are known to interfere with the ADME of drugs, such as previous surgery on the gastrointestinal tract (including removal of parts of the stomach, bowel, liver, gall bladder, or pancreas). Participants who have a history of appendectomy are eligible for enrollment.
History of chronic constipation, or recent complaints of an irregular defecation
Significant and/or acute illness at screening or within 5 days prior to study drug administration that may impact safety assessments, in the opinion of the Investigator.
Known personal or family history of congenital long QT syndrome or known family history of sudden death.
Participation in another ADME study with a radiation burden >0.1 mSv in the period of 1 year prior to screening.

View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT05718687). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.