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Tebipenem HBr

Phase 3

Complicated Urinary Tract Infection | Small molecule | Infectious Disease |Spero Therapeutics, Inc.|Last Updated: Mar 10, 2026

Target and mechanism

ModalitySmall molecule

Also known as TBPM-PI-HBr, Tebipenem pivoxil hydrobromide (TBPM-PI-HBr) - Reference, Tebipenem pivoxil hydrobromide- Reference, TBP-PI-HBr, Tebipenem pivoxil hydrobromide (TBPM-PI-HBr), Tebipenem pivoxil hydrobromide, SPR994

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindACTIVE_CONTROLLEDDMC
Total Trials1
Total Enrollment1,372

FDA Designations

No designations recorded

Clinical trial landscape

Tebipenem HBr · 11 trials · 6 indications

Phase 3 2Phase 1 9
NCT06059846A Study of Oral Tebipenem Pivoxil Hydrobromide (TBP-PI-HBr) Compared to Intravenous Imipenem-cilastatin in Participants With Complicated Urinary Tract Infection (cUTI) or Acute Pyelonephritis (AP)Urinary Tract Infection
COMPLETED1,690 Analytics
NCT03788967Study to Assess the Efficacy, Safety and Pharmacokinetics of Orally Administered Tebipenem Pivoxil Hydrobromide (SPR994) Compared to Intravenous Ertapenem in Participants With Complicated Urinary Tract Infection (cUTI) or Acute Pyelonephritis (AP)Complicated Urinary Tract Infection
COMPLETED1,372 Analytics
PHASE3COMPLETED
A Study of Oral Tebipenem Pivoxil Hydrobromide (TBP-PI-HBr) Compared to Intravenous Imipenem-cilastatin in Participants With Complicated Urinary Tract Infection (cUTI) or Acute Pyelonephritis (AP)
Urinary Tract InfectionUnlock trial analytics
PHASE3COMPLETED
Study to Assess the Efficacy, Safety and Pharmacokinetics of Orally Administered Tebipenem Pivoxil Hydrobromide (SPR994) Compared to Intravenous Ertapenem in Participants With Complicated Urinary Tract Infection (cUTI) or Acute Pyelonephritis (AP)
Complicated Urinary Tract InfectionUnlock trial analytics

Study Endpoints

Primary Endpoints

Number of Participants With Overall Response at the Test-of-Cure (TOC) Visit in the Microbiological Intent-to-Treat (Micro-ITT) Population
At Day 17 (TOC)

Overall response includes combined clinical cure plus microbiological eradication. Clinical cure is defined as a complete resolution or significant improvement of signs and symptoms of cUTI or AP present at baseline and no new symptoms, such that no further antibacterial therapy is warranted, and participant is alive. Microbiological eradication (favorable microbiological response) is defined as a reduction of baseline uropathogens to \<10\^3 CFU/mL and negative repeated blood culture if blood culture was positive for uropathogen growth at baseline and participant is alive.

Overall Response (Combined Clinical Cure and Microbiological Eradication) at Test-of-Cure (TOC) in Micro Intent-to-Treat Population
Day 19 (TOC)

Overall response is participants with combined clinical cure and microbiological eradication. Clinical cure is defined as complete resolution or significant improvement of signs and symptoms of cUTI or AP that were present at baseline and no new symptoms, such that no further antimicrobial therapy is warranted. Microbiological eradication is defined as reduction of baseline urine pathogen(s) to \<10\^3 colony forming unit/milliliter (CFU/mL) and negative repeated blood culture if blood culture was positive for uropathogen growth at baseline.

Number of Participants With Treatment Emergent Adverse Events (TEAEs) in The Safety Population
From the first dose of administration up to Day 25 post-treatment ± 2 days (up to approximately 27 days)

An Adverse Event (AE) was defined as any untoward medical occurrence in a subject or clinical investigation participant administered a pharmaceutical product, which does not necessarily have to have a causal relationship with the treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal (investigational/experimental) product, whether or not related to this product.

Part A and B: Maximum Observed Concentration (Cmax) of TBP in Plasma and Blood
Cohort 1: Pre-dose and at multiple timepoints post-dose up to Day 3; Cohort 2: Pre-dose and at multiple timepoints post-dose up to Day 5; Cohort 3: pre-dose and at multiple timepoints post-dose up to Day 7
Part A and B: Time to Cmax (Tmax) of TBP in Plasma and Blood
Cohort 1: Pre-dose and at multiple timepoints post-dose up to Day 3; Cohort 2: Pre-dose and at multiple timepoints post-dose up to Day 5; Cohort 3: pre-dose and at multiple timepoints post-dose up to Day 7
Part A and B: Area Under the Concentration-Time Curve (AUC) Extrapolated to Infinity [AUC(0-inf)] of TBP in Plasma and Blood
Cohort 1: Pre-dose and at multiple timepoints post-dose up to Day 3; Cohort 2: Pre-dose and at multiple timepoints post-dose up to Day 5; Cohort 3: pre-dose and at multiple timepoints post-dose up to Day 7
Part A and B: AUC From Time Zero to the Time of the Last Evaluable Concentration [AUC(0-t)] of TBP in Plasma and Blood
Cohort 1: Pre-dose and at multiple timepoints post-dose up to Day 3; Cohort 2: Pre-dose and at multiple timepoints post-dose up to Day 5; Cohort 3: pre-dose and at multiple timepoints post-dose up to Day 7
Part A and B: Amount Excreted in Urine (Ae) of TBP
Cohort 1: Pre-dose and at multiple timepoints post-dose up to Day 3; Cohort 2: Pre-dose and at multiple timepoints post-dose up to Day 5; Cohort 3: pre-dose and at multiple timepoints post-dose up to Day 7
Part A and B: Fraction of Dose Excreted in Urine (Fe) of TBP
Cohort 1: Pre-dose and at multiple timepoints post-dose up to Day 3; Cohort 2: Pre-dose and at multiple timepoints post-dose up to Day 5; Cohort 3: pre-dose and at multiple timepoints post-dose up to Day 7
Part B: AUC From Time Zero to 6 Hours Post-dose AUC(0-6) of TBP in Plasma and Blood
Pre-dose and at multiple timepoints post-dose up to Day 7
Part B: Ae of SPR1349
Pre-dose and at multiple timepoints post-dose up to Day 7
Part B: Fe of SPR1349
Pre-dose and at multiple timepoints post-dose up to Day 7
Percentage of Tebipenem (TBP) Samples With Converted (From Whole Blood Measurements) and Measured Plasma Concentrations That Have a Difference not Exceeding ±20% of the Mean of the Concentrations
Pre dose and at multiple time points post dose on Day 1
Area Under the Plasma Concentration-time Curve Extrapolated to Infinity (AUC0-∞) of TBP
Pre dose and at multiple time points post dose on Day 1
Maximum Plasma Concentration (Cmax) of TBP
Pre dose and at multiple time points post dose on Day 1
Plasma PK and lung penetration of SPR859 following multiple doses
Day 1 to Day 3

Plasma PK parameters will include the area under the curve (AUC) from time zero to the last quantifiable sample (AUC0-t), AUC from time zero to end of dosing interval (AUC0-8). The AUC0-8 values for ELF and AM will be determined. The ratios of the AUC0-8 of ELF to the AUC0-8 of plasma and the AUC0-8 of AM to the AUC0-8 of plasma will be calculated.

Pharmacokinetics (PK) of Tebipenem (TBPM) will be determined following administration of [14C]-TBPM-PI-HBr to healthy male subjects
Day 1 to Day 5

The primary PK outcome endpoints following oral administration of \[14C\]-TBPM-PI-HBr will be derived for TBPM in plasma (calculated from whole blood concentrations) based on the concentration-time profile

Total radioactivity will be determined following administration of [14C]-TBPM-PI-HBr to healthy male subjects
Day 1 to Day 5

The primary PK outcome endpoints following oral administration of \[14C\]-TBPM-PI-HBr will be derived for total radioactivity in whole blood and plasma based on the total radioactivity concentration-time profile

Area under the concentration-time curve, from time 0 to the last observed non-zero concentration (t).
Day 2 (Periods 1 and 2) and Day 6 (Period 3)
Area under the curve extrapolated to infinity (AUC0-∞).
Day 2 (Periods 1 and 2) and Day 6 (Period 3)
Percent of AUC0-inf extrapolated (AUC%extrap)
Day 2 (Periods 1 and 2) and Day 6 (Period 3)
Maximum plasma concentration (Cmax).
Day 2 (Periods 1 and 2) and Day 6 (Period 3)
Time to the maximum plasma concentration (Tmax).
Day 2 (Periods 1 and 2) and Day 6 (Period 3)
Terminal elimination half-life (t½).
Day 2 (Periods 1 and 2) and Day 6 (Period 3)
Apparent total body clearance (CL/F)
Day 2 (Periods 1 and 2) and Day 6 (Period 3)
Apparent volume of distribution during the terminal elimination phase after oral (extravascular) administration (Vz/F).
Day 2 (Periods 1 and 2) and Day 6 (Period 3)
Area under the concentration-time curve, from time 0 to the last observed non-zero concentration (t) (AUC0-t).
24h (Day 2) post dose (Arms: A, B, C)
Changes in the number of microorganisms in the intestinal flora of healthy subjects during and after 10 days of oral administration of TBPM-PI-HBr or amoxicillin-clavulanate
Change from baseline (Day-1), at Days 2, 4, 7, 10, 14, 21, 90, and 180

Changes in the number of microorganisms identified in feces

Changes in the types of microorganisms in the intestinal flora of healthy subjects during and after 10 days of oral administration of TBPM-PI-HBr or amoxicillin-clavulanate
Change from baseline (Day-1), at Days 2, 4, 7, 10, 14, 21, 90, and 180

Changes in the types of microorganisms identified in feces

Apparent total body clearance (CL/F).
72 hours post dose
Area under the curve from time zero to the last quantifiable sample (AUC0-last).
72 hours post dose
Apparent steadystate volume of distribution (Vss/F).
72 hours post dose
Terminal elimination half-life (t1/2).
72 hours post dose
Safety measures: adverse events
SAD: 1 to 7 days or 1 to 13 (food effect cohort); MAD 1 to 20 days

The incidence and severity of AEs

Safety measures: concomitant medications
SAD: 1 to 7 days or 1 to 13 (food effect cohort); MAD: 1 to 20 days

The type and frequency of medications used

Safety measures: physical examination
SAD: -1 to 7 days or -1 to 13 (food effect cohort); MAD: -1 to 20 days

Change from baseline to end of study visit

Safety measures: weight
SAD: -1 to 7 days or -1 to 13 (food effect cohort); MAD: -1 to 20 days

Change from baseline to end of study visit

Safety measures: pulse rate
SAD: -1 to 7 days or -1 to 13 (food effect cohort); MAD: -1 to 20 days

Change from baseline to end of study visit

Safety measures: ECG
SAD: -1 to 7 days or -1 to 13 (food effect cohort); MAD: -1 to 20 days

Change from baseline to end of study visit

Safety measures: clinical laboratory testing
SAD: -1 to 7 days or -1 to 13 (food effect cohort); MAD: -1 to 20 days

Change from baseline to end of study visit

Safety measures: respiratory rate
SAD: -1 to 7 days or -1 to 13 (food effect cohort); MAD: -1 to 20 days

Change from baseline to end of study visit

Safety measures: blood pressure
SAD: -1 to 7 days or -1 to 13 (food effect cohort); MAD: -1 to 20 days

Change from baseline to end of study visit

Safety measures: body temperature
SAD: -1 to 7 days or -1 to 13 (food effect cohort); MAD: -1 to 20 days

Change from baseline to end of study visit

Secondary Endpoints

Number of Participants With Overall Response (Combined Per-Participant Clinical Cure and Favorable Microbiological Response) at the TOC Visit in the Microbiologically Evaluable (ME) Population
At Day 17 (TOC)
Number of Participants With Overall Response at the End-of-Treatment (EOT) and Late Follow-Up (LFU) Visits in the Micro-ITT Population
At Day 10 (EOT) and Day 28 (LFU)
Number of Participants With Overall Response at EOT and LFU Visits in the ME Population
At Day 10 (EOT) and Day 28 (LFU)
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Study Design & Arms

AllocationRANDOMIZED
MaskingTRIPLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
TBP-PI-HBrEXPERIMENTALParticipants received TBP-PI-HBr 600 milligrams (mg), two x 300mg film-coated tablets, orally (PO) and a dummy infusion intravenously (IV), every 6 hours (q6h) from Day 1 through Day 10. Participants with estimated baseline creatinine clearance (CrCl) greater than (\>) 30 millilitres per minute (mL/min) and less than or equal to (≤) 50 mL/min received TBP-PI-HBr 300 mg q6h.
Imipenem-cilastatinACTIVE_COMPARATORParticipants received imipenem-cilastatin 500 mg, IV and matched dummy tablets, PO, q6h from Day 1 through Day 10. Dose adjustments for imipenem-cilastatin were made for participants with estimated baseline CrCl less than (\<) 90mL/min per approved imipenem-cilastatin package insert. Participants with baseline CrCl levels greater than or equal to (≥) 60 to \< 90 mL/min were administered imipenem-cilastatin, 400 mg IV q6h and participants with baseline CrCl levels \>30 to \<60 mL/min, were administered 300mg IV, q6h.
TBPM-PI-HBr 600 mgEXPERIMENTALTBPM-PI-HBr 600 mg (300 mg×2 ) film-coated tablets, administered orally three times per day (every 8 hours \[q8h\] ± 0.5 h) plus a single dummy IV infusion over 30 minutes (min) once daily (every 24 hours \[q24h\] ± 0.5 h) up to Day 15; participants with moderate renal insufficiency (creatinine clearance \[CrCl\] \>30 to ≤50 mL/min) required TBPM-PI-HBr dosage adjustment to 300 mg (one tablet) q8h ± 0.5 h.
Ertapenem 1 gACTIVE_COMPARATORErtapenem for IV injection, administered as a 1-gram IV infusion over 30 min once daily (q24h ± 0.5 h) plus dummy placebo tablets administered orally q8h (±0.5 h) up to Day 14; no dose adjustment of ertapenem was required for participants with renal insufficiency.
Part A: Cohort 1EXPERIMENTALParticipants will receive TBP-PI-HBr, 900 milligrams (mg) tablets orally, as a single dose under fasted condition on Day 1.
Part A: Cohort 2 (Fasted/Fed)EXPERIMENTALParticipants will receive TBP-PI-HBr, 1200 mg, tablets, orally, as a single dose under fasted and fed conditions on Day 1 and Day 3, as per the assigned crossover sequence.
Part B: Cohort 3EXPERIMENTALParticipants will receive TBP-PI-HBr, 600 mg, orally as a single dose on Day 1, followed by 9 doses every 6 hours from Day 3 through Day 5. (first and ninth dose will be given under fasted conditions).
TBP-PI-HBr 600 mgEXPERIMENTALHealthy participants meeting eligibility criteria will receive a single oral dose of TBP-PI-HBr 600 mg tablets (2 x 300 mg) on Day 1 under fasted conditions.
TBPM-PI-HBrEXPERIMENTALHealthy subjects meeting eligibility criteria will receive a total of five doses of TBPM-PI-HBr 600 mg orally every 8 hours.
TBPM-PI-HBr Alone (Period 1)EXPERIMENTALTebipenem pivoxil hydrobromide (TBPM-PI-HBr) 600 mg single-dose given orally alone.
TBPM-PI-HBr and Antacid (Period 2)EXPERIMENTAL20 mL aluminum hydroxide/magnesium hydroxide/simethicone (400 mg aluminum hydroxide/400 mg magnesium hydroxide/40 mg simethicone per 5 mL) oral suspension will be coadministered with 600 mg (2 x 300 mg tablets) TBPM-PI-HBr at Hour 0 on Day 1.
TBPM-PI-HBr and Omeprazole (Period 3)EXPERIMENTAL40 mg (1 x 40 mg capsule) omeprazole administered QD at Hour -2 on Days 1 through 5, with 600 mg (2 x 300 mg tablets) TBPM-PI-HBr administered at Hour 0 on Day 5.
A: TBPM-PI-HBr (Reference - fasted)EXPERIMENTAL600 mg (2 x 300 mg tablets) clinical study drug product batch TBPM-PI-HBr administered at Hour 0 on Day 1, under fasted conditions.
B: TBPM-PI-HBr (Test - fasted)EXPERIMENTAL600 mg (2 x 300 mg tablets) registration drug product batch TBPM-PI-HBr administered at Hour 0 on Day 1, under fasted conditions.
C: TBPM-PI-HBr (Test - fed)EXPERIMENTAL600 mg (2 x 300 mg tablets) registration drug product batch TBPM-PI-HBr administered at Hour 0 on Day 1, under fed conditions.
amoxicillin-clavulanateACTIVE_COMPARATORHealthy subjects meeting eligibility criteria will be sequentially randomized to receive either 500/125mg amoxicillin-clavulanate PO q8h (±1 hour) or 600mg TBPM-PI-HBr every 8 hours (PO q8h \[±1 hour\]) or for 10 days.
Tebipenem pivoxil hydrobromide (TBPM-PI-HBr)EXPERIMENTALTebipenem pivoxil hydrobromide (TBPM-PI-HBr) 600 mg single-dose given orally.
SPR994, FI, F2, F3, F4 Oral TabletsEXPERIMENTALSPR994 is active against multidrug-resistant Gram-negative and Gram-positive pathogens that cause serious and life-threatening infections, including extended spectrum beta-lactamase (ESBL) producers as well as strains resistant to levofloxacin and trimethoprim/sulfamethoxazole. SPR994 is administered in tablet form orally. Up to five different time released formulations of SPR994 will be studied in this protocol at 100 mg, 300 mg, 600 mg and 900 mg dosages. SAD Cohorts: One dose (two for food effect cohort) MAD Cohorts: Twenty-seven (27) doses administered twice daily (BID) over a period of 14 days or forty doses administered three times daily (TID) over period of 14 days
Placebo Oral TabletPLACEBO_COMPARATORPlacebo tablets (100, 300, and 600 mg) are pressed from a single placebo blend consisting of the same inactive ingredients; the active pharmaceutical ingredient (API) is replaced by Mannitol 200SD. SAD Cohorts: One dose (two for food effect cohort) MAD Cohorts: Twenty-seven (27) doses administered BID over a period of 14 days or forty doses administered TID over a period of 14 days
Optional Orapenem Open-Label ControlOTHERA single, optional, open-label, control cohort that may enroll, in which all 8 subjects receive Orapenem. SAD Cohort: One dose under fasted conditions and one dose under fed conditions.

Interventions

NameTypeDescription
TBP-PI-HBrDRUGTBP-PI-HBr film-coated immediate-release tablets.
Imipenem-cilastatinDRUGSterile powder for reconstitution administered as IV.
Dummy InfusionDRUG0.9% sodium chloride administered as IV infusion.
Dummy TabletsDRUGTBP-PI-HBr matching dummy tablets.
TBPM-PI-HBrDRUGTBPM-PI-HBr tablets administered orally.
ErtapenemDRUGAntibiotic Therapy for cUTI.
Tebipenem pivoxil hydrobromide (TBPM-PI-HBr)DRUGTebipenem pivoxil hydrobromide (TBPM-PI-HBr) 600 mg single-dose given orally.
20 mL aluminum hydroxide/magnesium hydroxide/simethicone (400 mg aluminum hydroxide/400 mg magnesium hydroxide/40 mg simethicone per 5 mL)DRUG20 mL aluminum hydroxide/magnesium hydroxide/simethicone (400 mg aluminum hydroxide/400 mg magnesium hydroxide/40 mg simethicone per 5 mL) oral suspension.
OmeprazoleDRUG40 mg (1 x 40 mg capsule) omeprazole administered QD
Tebipenem pivoxil hydrobromide (TBPM-PI-HBr) - ReferenceDRUG600 mg (2 x 300 mg tablets) clinical study drug product batch TBPM-PI-HBr.
Tebipenem pivoxil hydrobromide (TBPM-PI-HBr) - TestDRUG600 mg (2 x 300 mg tablets) registration drug product batch TBPM-PI-HBr.
amoxicillin-clavulanateDRUGamoxicillin-clavulanate (1 × 500mg/125mg tablet) PO q8h \[±1 hour\] for 10 days
SPR994DRUGSAD: Double-blind dosing will occur in all SAD Cohorts except for Cohort 12. In each cohort, six subjects will receive one of five different timed release formulations of SPR994 and 2 subjects will receive placebo. Subjects in SAD Cohorts 2, 3, 6, 16 and 17 will receive a single dose following a 10-h fast. Subjects in SAD Cohorts 1, 8-15 will receive one dose of SPR994 or placebo following a 10-h fast on Day 1 and a second dose following consumption of a standardized meal on Day 7. The dose escalation steps may be altered following review of the safety data of each cohort. MAD: Double-blind dosing will occur in all MAD Cohorts. Subjects will receive multiple doses of an optimal timed release formulation of SPR994 in MAD Cohort 4 (300 mg) and Cohort 5 (600 mg) or placebo for 14 consecutive days at either BID or TID dosing beginning on Day 1.
Placebo Oral TabletDRUGMannitol 200SD SAD: Two subjects in each cohort will receive matching placebo. MAD: Two participants in each cohort will receive matching placebo.
Orapenem®DRUGTebipenem pivoxil granules
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites85

Inclusion Criteria: 1. Have a diagnosis of cUTI or AP. 2. Have an adequate urine specimen for evaluation and culture obtained within 24 hours prior to randomization with evidence of pyuria that includes at least one of the following: 1. at least 10 white blood cells (WBCs) per high power field ...

Countries:United StatesArgentinaBosnia and HerzegovinaBrazilBulgariaCroatiaEstoniaGeorgiaGreeceHungaryIndiaLatviaMoldovaPolandRomaniaSerbiaSlovakiaSouth AfricaTurkey (Türkiye)CzechiaRussiaUkraineSwedenAustralia
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Frequently asked questions about Tebipenem HBr

What is Tebipenem HBr?

Tebipenem HBr is an oral small-molecule antibiotic being developed by Spero Therapeutics for infectious disease indications, including complicated urinary tract infection. It is an investigational drug that has completed Phase 3 clinical testing.

What is Tebipenem HBr used for?

Tebipenem HBr is being developed to treat complicated urinary tract infections, including acute pyelonephritis, and has also been studied in healthy participants and in people with renal impairment. It is an oral antibiotic intended for infections that are often treated with intravenous antibiotics.

Who makes Tebipenem HBr?

Tebipenem HBr is developed by Spero Therapeutics, Inc., which trades under the ticker SPRO. Spero is the sponsor of the clinical program for the drug.

What phase is Tebipenem HBr in?

Tebipenem HBr has completed Phase 3 clinical development. Seven trials have been completed, including a Phase 3 study in complicated urinary tract infection or acute pyelonephritis, and no trials are currently active. It is an investigational drug and is not approved by the FDA.

What clinical trials is Tebipenem HBr in?

Tebipenem HBr has been studied in completed trials including NCT06059846, a Phase 3 trial comparing oral TBP-PI-HBr to intravenous imipenem-cilastatin in complicated urinary tract infection or acute pyelonephritis, and Phase 1 trials NCT06727136, NCT05856747, and NCT04710407.

Is Tebipenem HBr the same as SPR994?

Yes, Tebipenem HBr is also known as SPR994, TBP-PI-HBr, and tebipenem pivoxil hydrobromide (TBPM-PI-HBr). These names refer to the same oral antibiotic candidate developed by Spero Therapeutics.