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Also known as Idasanutlin, RO5503781
RG7388 · 5 trials · 4 indications
| Arm | Type | Description |
|---|---|---|
| Treatment Sequence 1: ABCD | EXPERIMENTAL | Treatment A: A single dose of the current idasanutlin tablet A formulation (reference variant) on Cycle 1, Day 1 (one cycle is 28 days). Treatment B: A single dose of new idasanutlin tablet B (to investigate BE compared to tablet A) on Cycle 1, Day 8. Treatment C: A single dose of new idasanutlin tablet C (to investigate rBA compared to tablet A; rBA 1) on Cycle 1, Day 15. Treatment D: A single dose of new idasanutlin tablet D (to investigate rBA compared to tablet A; rBA 2) on Cycle 1, Day 22. Following completion of the BE/rBA cycle (Cycle 1), participants may continue to receive optional treatment cycles of the reference tablet formulation of idasanutlin, as specified in the Optional Treatment Extension Arm description. |
| Treatment Sequence 2: ABDC | EXPERIMENTAL | Treatment A: A single dose of the current idasanutlin tablet A formulation (reference variant) on Cycle 1, Day 1 (one cycle is 28 days). Treatment B: A single dose of new idasanutlin tablet B (to investigate BE compared to tablet A) on Cycle 1, Day 8. Treatment D: A single dose of new idasanutlin tablet D (to investigate rBA compared to tablet A; rBA 2) on Cycle 1, Day 15. Treatment C: A single dose of new idasanutlin tablet C (to investigate rBA compared to tablet A; rBA 1) on Cycle 1, Day 22. Following completion of the BE/rBA cycle (Cycle 1), participants may continue to receive optional treatment cycles of the reference tablet formulation of idasanutlin, as specified in the Optional Treatment Extension Arm description. |
| Treatment Sequence 3: BACD | EXPERIMENTAL | Treatment B: A single dose of new idasanutlin tablet B (to investigate BE compared to tablet A) on Cycle 1, Day 1 (one cycle is 28 days). Treatment A: A single dose of the current idasanutlin tablet A formulation (reference variant) on Cycle 1, Day 8. Treatment C: A single dose of new idasanutlin tablet C (to investigate rBA compared to tablet A; rBA 1) on Cycle 1, Day 15. Treatment D: A single dose of new idasanutlin tablet D (to investigate rBA compared to tablet A; rBA 2) on Cycle 1, Day 22. Following completion of the BE/rBA cycle (Cycle 1), participants may continue to receive optional treatment cycles of the reference tablet formulation of idasanutlin, as specified in the Optional Treatment Extension Arm description. |
| Treatment Sequence 4: BADC | EXPERIMENTAL | Treatment B: A single dose of new idasanutlin tablet B (to investigate BE compared to tablet A) on Cycle 1, Day 1 (one cycle is 28 days). Treatment A: A single dose of the current idasanutlin tablet A formulation (reference variant) on Cycle 1, Day 8. Treatment D: A single dose of new idasanutlin tablet D (to investigate rBA compared to tablet A; rBA 2) on Cycle 1, Day 15. Treatment C: A single dose of new tablet C (to investigate rBA compared to tablet A; rBA 1) on Cycle 1, Day 22. Following completion of the BE/rBA cycle (Cycle 1), participants may continue to receive optional treatment cycles of the reference tablet formulation of idasanutlin, as specified in the Optional Treatment Extension Arm description. |
| Optional Treatment Extension Arm | EXPERIMENTAL | Following completion of the BE/rBA cycle (Cycle 1), participants who have no clinically defined progressive disease per Response Evaluation Criteria in Solid Tumors version 1.1 (RECIST v1.1) and who recover from any prior treatment toxicity to Grade \</=1 may enter the optional treatment extension phase. Participants will receive 200 mg idasanutlin orally (200-mg tablet reference formulation) daily for 5 days, followed by 23 days of rest. This extension phase will continue for additional 28-day cycles or until disease progression or unacceptable toxicity is observed. |
| Idasanutlin | EXPERIMENTAL | On Day 1, 300 milligram (mg) idasanutlin tablet orally and 100 mg \[14C\]-radiolabeled idasanutlin capsule orally (2, 50 mg capsules containing approximately 100 microcurie of radioactivity). After 5 hours and 45 minutes of the oral dose, 100 microgram (mcg) of \[13C\]-radiolabeled idasanutlin will be administered over a 15-minute intravenous (IV) infusion. On Day 11, idasanutlin matching placebo aqueous dispersion orally and approximately after 1 hour, 400 mg idasanutlin tablet will be administered orally in the form of an aqueous dispersion. On Day 19, 400 mg idasanutlin tablet will be administered orally in the form of an aqueous dispersion. Participants, who are eligible to enter in optional treatment extension phase, will continue treatment with idasanutlin 200 mg tablet orally once daily for 5 days, and no treatment during 23 days of 28-day cycle, until the development of progressive disease, unacceptable toxicity, consent withdrawal or any other criteria for removal. |
| RG7388 | EXPERIMENTAL | Part A: RG7388 as a single agent; given at a starting dose of 100 mg each day for five days for the first cycle which will be 56 days. Part B: combination of RG7388 and Pegasys if subject does not achieve at least a PR by the end of 3 cycles of single agent RG7388 |
| Extension | EXPERIMENTAL | - |
| Part 1: Drug-drug interaction | EXPERIMENTAL | - |
| Part 2: Relative bioavailability | EXPERIMENTAL | - |
| Part 3: Food effect | EXPERIMENTAL | - |
| Schedule A: RO5503781 QW | EXPERIMENTAL | Participants will receive multiple ascending doses of RO5503781 orally once weekly (QW) x 3 followed by 13 days of rest in a 28 days cycle. |
| Schedule B: RO5503781 QD | EXPERIMENTAL | Participants will receive multiple ascending doses of RO5503781 orally QD x 5 followed by 13 days of rest in a 28 days cycle. |
| Name | Type | Description |
|---|---|---|
| Idasanutlin | DRUG | Participants will receive one 300-mg dose of each of the four different oral tablet formulations of idasanutlin (tablet A \[reference\], B, C, D) during Cycle 1, in the order specified for their assigned treatment arm (Treatment Sequence 1-4). Participants who enter the optional treatment extension phase will receive the reference tablet formulation of idasanutlin, as specified in the Optional Treatment Extension Arm description. |
| Placebo | DRUG | Placebo matching to idasanutlin aqueous dispersion will be administered orally on Day 11. |
| [13C]-radiolabeled Idasanutlin | DRUG | \[13C\]-radiolabeled idasanutlin 100 mcg will be administered as IV infusion over 15-minute on Day 1. |
| [14C]-radiolabeled Idasanutlin | DRUG | \[14C\]-radiolabeled idasanutlin 100 mg capsule (2, 50 mg capsules containing approximately 100 microcurie of radioactivity) will be administered orally on Day 1. |
| RG7388 | DRUG | RG7388 is supplied as film-coated tablets at dosage strengths of 50 mg, 200 mg, 300mg and 400 mg. |
| Pegasys | DRUG | PEGASYS is supplied as a clear, sterile solution for subcutaneous (SQ) injection available in prefilled syringes. weekly doses at 45ug subcutaneously |
| RO5503781 | DRUG | Single dose on Day 1 (high fat, low fat, or fasted), Day 10 (fasted, low fat, or high fat), and Day 19 (low fat, fasted, or high fat) in a crossover design |
| posaconazole | DRUG | Multiple doses Days 8-14 |
Inclusion Criteria: * Participant must have histologically or cytologically confirmed advanced malignancies, except all forms of leukemia and lymphoma, for which standard curative or palliative measures do not exist, are no longer effective, or are not acceptable to the participant * Measureable or...
Top 7 of 8 competitors
| Company | Ticker | Trials | Lead Phase | Drugs |
|---|---|---|---|---|
| Merck & Co., Inc. | MRK | 2 | PHASE3 | Bomedemstat |
| Protagonist Therapeutics, Inc. | PTGX | 2 | PHASE3 | Rusfertide |
| Disc Medicine, Inc. | IRON | 1 | PHASE2 | DISC-3405 |
| Takeda Pharmaceutical Co. Ltd. Sponsored ADR | TAK | 3 | PHASE2 | Rusfertide |
| Agios Pharmaceuticals, Inc. | AGIO | 1 | PHASE2 | AG-236 |
| Prelude Therapeutics, Inc. | PRLD | 1 | PHASE1 | PRT12396 |
| Silence Therapeutics PLC Sponsored ADR | SLN | 1 | PHASE1 | SLN124 |